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PsychedeliaDokholyan Laboratory
Plate 432 of 545Verified

Methysergide

Also known asMethysergid · Desernil · Deseril · 1-Methylmethylergonovine · Methysergidum · Metisergide · Metisergido · metisergida

(6aR,9R)-N-[(2S)-1-hydroxybutan-2-yl]-4,7-dimethyl-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-9-carboxamide

PubChem CID
9681
Measurements
224
InChIKey
KPJZHOPZRAFDTN-ZRGWGRIASA-N

I · Summary

What is known

Published passages, each quoted whole and attributed to the database that published it. Two blocks are written here rather than quoted, and both say so where they stand: the synthesized summary at the top, which may draw only on the passages beneath it, and the history note, which cites the works it came from. Every claim in either carries a marker to its source.

What it is

  • (6aR,9R)-N-[(2S)-1-hydroxybutan-2-yl]-4,7-dimethyl-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-9-carboxamide is an ergoline alkaloid.

    ChEBI

  • An ergot derivative that is a congener of lysergic acid diethylamide. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.

    DrugBank

  • See also: Methysergide Maleate (active moiety of); Methysergide Dimaleate (active moiety of).

    PubChem

Recognized use

  • For the prevention or reduction of intensity and frequency of vascular headaches in the following kinds of patients: Patients suffering from one or more severe vascular headaches per week; Patients suffering from vascular headaches that are uncontrollable or so severe that preventive therapy is indicated regardless of the frequency of the attack. /Included in US product label/

    Therapeutic Uses

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • ...Sometimes useful in suppression of GI hypermotility and spasm and cardiovascular disorders that occur in patients with carcinoid tumor. These tumors release large amounts of serotonin into blood stream, and antiserotonin actions of drug are responsible for beneficial effects. ...Some benefit in attenuating dumping syndrome. /Maleate/

    Therapeutic Uses

    Hazardous Substances Data Bank (HSDB)Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 877

  • Methysergide is a synthetic derivative of the ergoline family, which occur naturally in various species of vines of the Convolvulaceae (morning glory) family and in some species of lower fungi like other ergoline alkaloids. Methysergide antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. It is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome and is sold under the brand names Sansert and Deseril in 2mg dosages. (L1918, L1924)

    Use Classification

    Toxin and Toxin Target Database (T3DB)

How it acts

  • Methysergide is serotonin antagonists acts on central nervous system (CNS), which directly stimulates the smooth muscle leading to vasoconstriction. Some alpha-adrenergic blocking activity has been reported. Suggestions have been made by investigators as to the mechanism whereby Methysergide produces its clinical effects, but this has not been finally established, although it may be related to the antiserotonin effect.

    DrugBank

  • Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain threshold (others in this category include tyramine; polypeptides, such as bradykinin; histamine; and acetylcholine), as an intrinsic "motor hormone" of the gastrointestinal tract, and as a "hormone" involved in connective tissue reparative processes. Suggestions have been made by investigators as to the mechanism whereby methysergide produces its clinical effects…

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

Behavior carries the pharmacological classes and the acute-effect durations, with plasma half-life kept separate from duration of effect.

In the body

  • Five healthy men were given 1.0 mg methysergide maleate intravenously and 2.7 mg methysergide maleate orally in a cross-over study. The systemic availability of methysergide was only 13%, most probably due to a high degree of first-pass metabolism to methylergometrine. We also found evidence of extrahepatic clearance of methysergide. After oral administration the plasma concentrations of the metabolite were considerably higher than those of the parent drug and the area under the plasma concentration curve (AUC) for methylergometrine was more than ten times greater than for methysergide. /These/ findings may be relevant to the treatment of migraine if methylergometrine contributes to the effe…

    Hazardous Substances Data Bank (HSDB)PMID 3709634Bredberg U et al; Eur J Clin Pharmacol 30 (1): 75-7 (1986)

  • The pharmacokinetics of methysergide (MS) and its metabolite methylergometrine (MEM) was studied in male Sprague-Dawley rats. MS was administered iv in doses of 0.71 (0.25 mg/kg) or 2.8 mumol/kg (1.0 mg/kg). The metabolite MEM was administered as iv doses of 0.74 (0.25 mg/kg) or 2.9 mumol/kg (1.0 mg/kg). The steady state characteristics of these compounds were also studied after constant rate iv infusion of MS at two different rates, 0.70 and 14.0 nmol/min per kg. Plasma protein binding and blood/plasma partitioning for MS were determined over a range of concentrations. Plasma and blood concentrations of MS and MEM were measured by HPLC with fluorescence detection. The plasma clearance of MS…

    Hazardous Substances Data Bank (HSDB)PMID 1974196Bredberg U, Paalzow L; Drug Metab Dispos 18 (3): 338-43 (1990)

  • About 30% of oral dose of (N-methyl-(14)C)-methysergide was excreted in 48-hr urine and about 50% in expired air of human subjects. Excretion of (14)C was maximal 2 hr after dosing, and excretion of (14)C in expired air (as (14)CO2) was almost complete in 8 hr.

    Hazardous Substances Data Bank (HSDB)The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 2: A Review of the Literature Published Between 1970 and 1971. London: The Chemical Society, 1972., p. 78

History, discovery and cultural use

— Not in this archive. PubChem, ChEMBL and the Human Protein Atlas publish pharmacology, regulation and toxicology, and none of them publishes a heading for when Methysergide was first made, by whom, or how it has been used. That is a gap in the databases this site reads and not a gap in the literature — the history of these compounds is written, at length and under peer review, in the works below. This site does not summarize them; it says where they are. Where a published passage above happens to touch origin or traditional use, it appears inside the entry that carries it.

Histories of this field

Scholarship on psychedelics generally, not on Methysergide specifically. Whether any of these treats this compound is a question for the book, not for this page.

  • Mescaline: A Global History of the First Psychedelic

    Traces mescaline and the peyote and San Pedro cacti from pre-Columbian ritual use through nineteenth-century chemistry to twentieth-century psychiatry and the counterculture.

    Jay M. Mescaline: A Global History of the First Psychedelic. Yale University Press, New Haven and London; 2019. ISBN 9780300231076.

  • Expanding Mindscapes: A Global History of Psychedelicsopen access

    Essays on the international and cross-cultural history of psychedelic science, deliberately decentring the standard North American and European account.

    Dyck E, Elcock C, editors. Expanding Mindscapes: A Global History of Psychedelics. The MIT Press, Cambridge MA; 2023. ISBN 9780262546935 (paper), 9780262376891 (open access). doi:10.7551/mitpress/14417.001.0001.

  • Plants of the Gods: Their Sacred, Healing, and Hallucinogenic Powers

    Botany, ethnography and chemistry of the principal hallucinogenic plants, by the founder of modern ethnobotany and the chemist who first synthesized LSD.

    Schultes RE, Hofmann A, Rätsch C. Plants of the Gods: Their Sacred, Healing, and Hallucinogenic Powers. 2nd ed. Healing Arts Press, Rochester VT; 2001. ISBN 9780892819799.

  • Psychonauts: Drugs and the Making of the Modern Mind

    The tradition of scientific self-experimentation with psychoactive drugs, and its part in the emergence of psychology and of modernism.

    Jay M. Psychonauts: Drugs and the Making of the Modern Mind. Yale University Press, New Haven; 2023. ISBN 9780300257946.

  • Ancient Psychoactive Substances

    Archaeological and bioarchaeological evidence for psychoactive plant use across the ancient world.

    Fitzpatrick SM, editor. Ancient Psychoactive Substances. University Press of Florida, Gainesville; 2018. ISBN 9780813056708.

  • History and Current Status of Psychedelics and Entactogens for the Treatment of Psychiatric Disorders

    A chapter tracing psychedelic and entactogen research from earlier ritual use through the mid-century research period to current clinical trials.

    Stroud C, Posey Norris SM, Matney C, editors. History and Current Status of Psychedelics and Entactogens for the Treatment of Psychiatric Disorders. In: Exploring Psychedelics and Entactogens as Treatments for Psychiatric Disorders: Proceedings of a Workshop. National Academies Press, Washington DC; 2022. NBK587225.

    Workshop proceedings record what participants said; they are not a consensus statement of the National Academies.

  • Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic Repercussions

    Peer-reviewed review covering the isolation, synthesis, pharmacology and ritual use of peyote and mescaline.

    Dinis-Oliveira RJ, Pereira CL, da Silva DD. Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic Repercussions. Current Molecular Pharmacology 12(3):184–194; 2019. doi:10.2174/1874467211666181010154139.

Institutional archives

  • Heffter Research Institute Funds and coordinates clinical research on psilocybin, and keeps records of the studies it has supported since 1993. Sponsors the research it archives.
  • Multidisciplinary Association for Psychedelic Studies (MAPS) Sponsors clinical research, chiefly on MDMA-assisted therapy, and publishes an archive of historical and contemporary documents. A sponsor and an advocacy organization, not a disinterested archive; its clinical programme has a commercial arm.

The rest of this dossier

  • Affinity — 224 measurements in this archive, equilibrium constants kept apart from functional readouts.
  • Toxicology — 11 published passages, plus any assay in this archive bearing on toxicity.
  • Legal — no DEA record is held here — which is not a finding that this compound is uncontrolled.
  • Systems — where this compound’s targets are transcribed, by brain region and tissue.

Passages via PubChem descriptive sections, aggregating DrugBank, LiverTox, FDA, DEA, HSDB, EPA. Each is quoted whole and attributed to the database that published it. The only prose written here about Methysergide is the history note, which says so on its face and carries a reference for every claim in it.

II · Identity

Structure and descriptors

Descriptors are computed here with RDKit from the structure PubChem returns — not from the archive's stored copy, so an edited local structure cannot reach this table.

2D structural depiction of Methysergide
Depiction served by PubChem for CID 9681. Not redrawn here, so the picture and the identity come from the same record.
Formula
C21H27N3O2R
Molecular weight
353.47g/molR
Exact mass
353.2103DaR
cLogP
1.94R
TPSA
57.5ŲR
H-bond donors
2R
H-bond acceptors
4R
Rotatable bonds
4R
Aromatic rings
2R
Heavy atoms
26R
Fraction sp³
0.476R
Formal charge
0R

Computed with RDKit 2025.09.2 from the SMILES returned by PubChem. Audit run 26/09/2026.

Bemis–Murcko scaffold

C1=C2c3cccc4[nH]cc(c34)C[C@H]2NCC1

Shared with 1B-LSD, 1DD-LSD, 1H-LSD, 1P-AL-LAD, 1P-ETH-LAD, 1P-LSD and 23 more. All families

III · Behavior

Behavioral summary

Class, mechanism, and the duration of acute effects — each quoted from the record or trial that publishes it. Duration of effects and plasma half-life are shown separately, because they are different quantities and diverge by a factor of three or four.

Classification

Duration of acute subjective effects

—

No controlled human trial reporting a duration for this compound is cited here. The archive holds no other record of one either. A duration is not inferred from a chemical relative.

Plasma elimination half-life

How fast the body clears the drug — not how long the effects last. The two diverge sharply: LSD is cleared with a half-life of about 2.6 h while its subjective effects run 8–12 h.

  • Five healthy men were given 1.0 mg methysergide maleate intravenously and 2.7 mg methysergide maleate orally in a cross-over study. ... Methylergometrine had a significantly longer elimination half-life than methysergide (223 +/- 43 min vs 62.0 +/- 8.3 min and 174 +/- 35 min vs 44.8 +/- 8.1 min in the oral and intravenous studies respecti…
    Hazardous Substances Data Bank (HSDB)PMID 3709634Bredberg U et al; Eur J Clin Pharmacol 30 (1): 75-7 (1986)

Primary pharmacological drivers

ChEMBL holds no curated mechanism-of-action record for this compound. The measured affinities below are the evidence this archive has for what it binds.

Mechanism, as published

Quoted verbatim from the database named after each passage, never summarized.

  • ... Here /investigators/ asked whether systemic (i.p.) and intrathecal (i.t.) administrations of a nonselective serotonergic antagonist, methysergide, might produce paradoxical antinociception similar to naloxone in the mouse formalin test. A diluted formalin solution was injected into the mouse plantar region of the hind paw and the dura…
    Hazardous Substances Data Bank (HSDB)PMID 12928583Chung KM et al; Pharmacology 69 (2): 93-101 (2003)
  • Methysergide is serotonin antagonists acts on central nervous system (CNS), which directly stimulates the smooth muscle leading to vasoconstriction. Some alpha-adrenergic blocking activity has been reported. Suggestions have been made by investigators as to the mechanism whereby Methysergide produces its clinical effects, but this has not…
    DrugBank
  • Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain thresh…
    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4
  • Considering structure/effect relationships, it has been demonstrated that methylation of the indole nitrogen in the lysergic acid ring of the alkanolamides fundamentally alters their pharmacologic behavior and is associated with inhibition or blockade of a great variety of serotonin-induced effects...
    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4
  • Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain thresh…
    DrugBank

IV · Clinical

Clinical description

Where this compound's substance class sits in ICD-11 and DSM-5-TR, and how much of the recorded literature speaks to each domain of a mental status examination.

No diagnostic chapter is shown for this compound. Either PubChem records no MeSH pharmacological class for it, or the class it records is not one of the substance classes ICD-11 gives a chapter to. Inferring a chapter from the compound’s name or its binding profile would be a diagnosis this archive is in no position to make.

How much has been written about each domain

The clinical domains, and how many of the records this archive holds for this compound say something under each. What the terms mean, and the word list behind every spoke, are set out in the method.

Affect0Mood2Perception1Cognition2Thought process0Thought content0Psychomotor activity1Insight and judgment0
This measures the literature, not the compound. Each spoke counts how many of the 17 records this archive holds for this compound say something under that domain — 2 at the widest ring. A long spoke means the subject has been written about, not that the effect is strong, and a spoke at the center means nothing here discusses it rather than that nothing happens. The terms behind each domain are listed in the method.
Mood 2
matched on “elation”, “euphoria” · in Pharmacology: Mechanism of Action; Toxicology: Hazardous Substances Data Bank (HSDB)
Perception 1
matched on “hallucinat” · in Toxicology: Toxin and Toxin Target Database (T3DB)
Cognition 2
matched on “attention”, “concentrat” · in PMID 7371695; PMID 9413296
Psychomotor activity 1
matched on “hyperactiv” · in Toxicology: Hazardous Substances Data Bank (HSDB)

V · Systems

Systems physiology

Where the targets this compound binds are transcribed — brain regions on the left, peripheral and autonomic tissues on the right. A join of two measurements, not a claim about what the compound does to either.

Brain

cerebral cortex — 18.6 nTPM, from CNR1, HTR2A, ADRA2Ccerebellum — 18.3 nTPM, from CNR1, ADRA2A, HTR5Ahippocampal formation — 13.2 nTPM, from CNR1, HTR1A, ADRA2Camygdala — 13.3 nTPM, from CNR1, ADRA2C, HTR2Ahypothalamus — 12.6 nTPM, from HTR2C, DRD2, CNR1thalamus — no resolved target expressed herebasal ganglia — 62.0 nTPM, from DRD2, HTR2C, DRD1medulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: pituitary gland 56.6, midbrain 23.4, retina 10.8, spinal cord 1.7.

Body

heart — 9.4 nTPM, from ADRA2B, ADRA2C, HTR2Bsmooth muscle — 15.7 nTPM, from HTR2B, ADRA2A, HTR2Alung — 27.2 nTPM, from SLC6A4, ADRA2A, ADRA2Cliver — 6.3 nTPM, from ADRA2B, HTR2B, ADRA2Akidney — 33.4 nTPM, from ADRA2C, ADRA2B, ADRA2Astomach — 4.7 nTPM, from HTR1B, HTR2B, ADRA2Aduodenum — 9.7 nTPM, from SLC6A4, ADRA2A, HTR1Dsmall intestine — 38.0 nTPM, from SLC6A4, CNR1, HTR1Dcolon — 10.0 nTPM, from CNR1, HTR2B, ADRA2Aadrenal gland — 17.2 nTPM, from HTR2B, DRD2, CNR1thyroid gland — 8.7 nTPM, from ADRA2A, CNR1, HTR2Bpancreas — 28.8 nTPM, from ADRA2A, ADRA2C, SLC6A4urinary bladder — 14.8 nTPM, from ADRA2A, ADRA2C, CNR1skeletal muscle — 6.0 nTPM, from ADRA2B, ADRA2C, CNR1spleen — 20.8 nTPM, from ADRA2C, ADRA2A, ADRA2Bsalivary gland — 11.3 nTPM, from DRD2, ADRA2A, ADRA2B
062 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of this compound’s resolved targets above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain regions

Regions where this compound's measured targets are transcribed. Linked from the plate above.

  1. basal ganglia

    62.0 nTPM

  2. pituitary gland

    56.6 nTPM

  3. midbrain

    23.4 nTPM

  4. cerebral cortex

    18.6 nTPM

  5. cerebellum

    18.3 nTPM

  6. amygdala

    13.3 nTPM

  7. hippocampal formation

    13.2 nTPM

  8. hypothalamus

    12.6 nTPM

  9. retina

    10.8 nTPM

  10. spinal cord

    1.7 nTPM

Peripheral & autonomic

Tissues outside the CNS expressing the same targets — where a compound's bodily effects become possible.

  1. small intestine

    38.0 nTPM

  2. kidney

    33.4 nTPM

  3. pancreas

    28.8 nTPM

  4. lung

    27.2 nTPM

  5. spleen

    20.8 nTPM

  6. adrenal gland

    17.2 nTPM

  7. smooth muscle

    15.7 nTPM

  8. urinary bladder

    14.8 nTPM

  9. salivary gland

    11.3 nTPM

  10. colon

    10.0 nTPM

  11. duodenum

    9.7 nTPM

  12. heart muscle

    9.4 nTPM

  13. thyroid gland

    8.7 nTPM

  14. liver

    6.3 nTPM

  15. skeletal muscle

    6.0 nTPM

  16. stomach 1

    4.7 nTPM

Each row joins two published measurements and nothing else: the affinity this archive holds for the compound at that target, and the transcript level the Human Protein Atlas reports for that target’s gene in that region. Bars scale with expression only. Expression is not activation — a receptor transcribed in a region is a receptor available to be bound there, which is a weaker and more defensible claim than saying the region is affected.

4 of this compound’s targets could not be resolved to a gene and are absent from both columns: 5-HT2, 5-HT5B, 5-HT7B, Sigma 1.

Expression data from Human Protein Atlas (CC BY-SA 3.0), RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset. Uhlén M, et al. Tissue-based map of the human proteome. Science. 2015;347(6220):1260419.

VI · Profile

Affinity rosette

The strongest measurement at each of 23 molecular targets. Cell-line and whole-organism screens are excluded here — they carry no affinity — and appear in the table below.

5-HT2B — Ki 10.00 pX5-HT2A — Ki 9.38 pX5-HT2C — Ki 9.10 pX5-HT1B — Ki 8.60 pX5-HT1D — Ki 8.44 pX5-HT2 — Ki 8.28 pX5-HT1F — Ki 8.20 pX5-HT7 — Ki 7.90 pX5-HT6 — Ki 7.90 pX5-HT1A — Ki 7.85 pX5-HT7B — Ki 7.57 pX5-HT5B — Ki 7.39 pX5-HT1E — Ki 7.23 pX5-HT5A — Ki 7.20 pXD3 — Ki 7.23 pXD2 — Ki 6.94 pXD1 — Ki 6.66 pXAlpha2C — Ki 7.05 pXAlpha2B — Ki 6.97 pXAlpha2A — Ki 6.77 pXSigma 1 — IC50 6.04 pXSERT — Ki 5.43 pXCB1 — Ki 7.20 pX5-HT2B5-HT2A5-HT2C5-HT1B5-HT1D5-HT25-HT1F5-HT75-HT65-HT1A5-HT7B5-HT5B5-HT1E5-HT5AD3D2D1Alpha2CAlpha2BAlpha2ASigma 1SERTCB1579
Fig. Radius is pX = −log₁₀(value in M), that is 9 − log₁₀(value in nM), computed from the normalized measurement. Hatched wedges are equilibrium binding constants (Ki, Kd); dashed outlines are functional readouts (IC₅₀, EC₅₀, AC₅₀, potency), which answer a different question and are not pooled with them. Rings mark whole pX units from 5 to 10, labeled every second ring in the gutter at the top. Where a target carries several measurements, the strongest is drawn.

VII · Toxicology

Toxicological profile

What has been measured, and what has been published — kept apart, and neither scored. There is no risk rating on this page; the archive once carried one, identical for every compound, produced by a stub.

Measured in this archive

Assays that bear on toxicity, drawn from the same ChEMBL records as everything else on this page. They are measurements of what a compound binds or does to cells — not verdicts about what it does to a person.

No hERG, cytochrome, cytotoxicity or transport measurement exists for Methysergide in this archive.

Lethal-dose values — animal studies

These are not human doses. An LD50 is the dose killing half of a group of animals of one species by one route, and it is a poor predictor of human risk for these compounds. Each value is printed whole, with the species and route it was measured in, because a lethal dose separated from those two facts is worse than no figure at all. Nothing here supports inferring a safe dose for anyone.

  • LD50 Rat oral 2100 mg/kg

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • LD50 Rat iv 125 mg/kg

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • LD50 Rabbit iv 28 mg/kg

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • LD50 Mouse iv 185 mg/kg

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • LD50 Mouse oral 581 mg/kg

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

As published

Quoted verbatim from the database named after each passage, never summarized — a summary of a toxicology statement is a new claim.

Toxicity Summary

  • Ergoline alkaloids have been shown to have the significant affinity towards the 5-HT1 and 5-HT2 serotonin receptors, D1 and D2 dopamine receptors, and alpha-adrenergic receptors. This can result in a number of different effects, including vasoconstriction, convulsions, and hallucinations. Methysergide as a serotonin antagonists acts on central nervous system, which directly stimulates the smooth muscle leading to vas…

    Toxin and Toxin Target Database (T3DB)

Human Toxicity Excerpts

  • /HUMAN EXPOSURE STUDIES/ The effects of acute oral administration of the antiserotoninergic drugs methysergide (3 mg) and metergoline (4 mg) on basal, submaximal (0.6 ug/kg i. m.) and maximal (6 ug/kg) pentagastrin-stimulated gastric acid secretion, as well as on basal and food-induced gastrin release, have been evaluated in healthy volunteers. Methysergide significantly increased basal and submaximal pentagastrin-st…

    Hazardous Substances Data Bank (HSDB)PMID 7371695Caldara R et al; Eur J Clin Pharmacol 17 (1): 13-8 (1980)

  • /SIGNS AND SYMPTOMS/ Few cases of acute Methysergide intoxication have been reported. The possible symptom complex is therefore not fully known. The following symptoms are based on these few case reports. Euphoria, hyperactivity, tachycardia, dilated pupils, and dizziness have been reported in a child with a dose of 20-24 mg of methysergide. In adults, peripheral vasospasm, with diminished or absent pulses, coldness,…

    Hazardous Substances Data Bank (HSDB)US Natl Inst Health; DailyMed. Current Medication Information for sansert (methysergide maleate) tablet, coated (February 2006). Available from, as of March 6, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3fae28ee-700e-4d4f-a040-02ef01a2aeb4

  • /CASE REPORTS/ Neuropathologic manifestations due to chronic ergotism are rare. /Investigators/ report the case of a 40-year-old patient who presented clinical signs and symptoms of a spinal lesion and also the symptoms of neuropathy involving the right sciatic nerve, more precisely the internal and external popliteal nerves, following ingestion of methysergide. Complete recovery was achieved with calcium blocker tre…

    Hazardous Substances Data Bank (HSDB)PMID 15454875Sallansonnet-Froment M et al; Rev Neurol (Paris) 160 (8-9): 843-5 (2004)

  • /CASE REPORTS/ A 25-year-old woman sought medical attention because of iliocaval manifestations of retroperitoneal fibrosis while she was taking methysergide. Laboratory studies yielded substantially increased serum procollagen III levels and anticardiolipin antibodies accompanied with anti-beta(2) glycoprotein I, findings not previously described with this disorder. Clinical and laboratory manifestations resolved af…

    Hazardous Substances Data Bank (HSDB)PMID 9413296Bucci JA, Manoharan A; Mayo Clin Proc 72 (12): 1148-50 (1997)

  • For more Human Toxicity Excerpts (Complete) data for METHYSERGIDE (18 total), please visit the HSDB record page.

    Hazardous Substances Data Bank (HSDB)

Published passages via PubChem toxicology sections, aggregating Hazardous Substances Data Bank (HSDB), RTECS, LiverTox. No figure on this page is scored, ranked or combined into a risk level.

VIII · Evidence

Every measurement

One row per published value. The identifier in the last column resolves to the ChEMBL assay record it was read from.

Equilibrium binding constants 210

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
5-HT2BSerotonin receptorsKi0.10010.00HUMANPDSP
5-HT2BSerotonin receptorsKi0.10010.00testPMID 28792478
5-HT2BSerotonin receptorsKi0.3589.45Homo sapiensCHEMBL1909104
5-HT2BSerotonin receptorsKi0.3639.44HUMANPMID 15322733
5-HT2ASerotonin receptorsKi0.4209.38RATPMID 8935801
5-HT2BSerotonin receptorsKi0.6409.19HUMANPMID 9459568
5-HT2CSerotonin receptorsKi0.8009.10RATPMID 9928251
5-HT2CSerotonin receptorsKi0.8009.10RATPMID 10611640
5-HT2ASerotonin receptorsKi0.9409.03RATPDSP
5-HT2CSerotonin receptorsKi0.9509.02HUMANPMID 9225287
5-HT2CSerotonin receptorsKi1.009.00RATPMID 9928251
5-HT2CSerotonin receptorsKi1.009.00RATPMID 10611640
5-HT2CSerotonin receptorsKi1.028.99RATPMID 9225287
5-HT2ASerotonin receptorsKi1.078.97RATPDSP
5-HT2ASerotonin receptorsKi1.078.97RATPMID 9225287
5-HT2CSerotonin receptorsKi1.098.96Homo sapiensCHEMBL1909105
5-HT2ASerotonin receptorsKi1.208.92RATPDSP
5-HT2CSerotonin receptorsKi1.268.90PIGPDSP
5-HT2ASerotonin receptorsKi1.308.89RATPMID 8584042
5-HT2BSerotonin receptorsKi1.518.82HUMANPMID 9459568
5-HT2ASerotonin receptorsKi1.588.80RATPMID 7582481
5-HT2CSerotonin receptorsKi1.588.80HUMANPMID 7582481
5-HT2ASerotonin receptorsKi1.588.80HUMANPMID 23043420
5-HT2BSerotonin receptorsKi1.598.80HUMANPMID 8632342
5-HT2ASerotonin receptorsKi1.608.80Rattus norvegicusCHEMBL617930
5-HT2BSerotonin receptorsKi1.658.78HUMANPMID 9225287
5-HT2CSerotonin receptorsKi1.808.74RATPMID 11104741
5-HT2CSerotonin receptorsKi1.808.74RATPDSP
5-HT2ASerotonin receptorsKi1.908.72RATPDSP
5-HT2CSerotonin receptorsKi1.998.70RATPMID 7582481
5-HT2ASerotonin receptorsKi2.008.70Rattus norvegicusCHEMBL617332
5-HT2CSerotonin receptorsKi2.008.70PIGPDSP
5-HT2CSerotonin receptorsKi2.008.70PIGPDSP
5-HT2CSerotonin receptorsKi2.008.70PIGPDSP
5-HT2CSerotonin receptorsKi2.008.70PIGPDSP
5-HT2ASerotonin receptorsKi2.248.65RATPDSP
5-HT2ASerotonin receptorsKi2.458.61HUMANPMID 9225287
5-HT2CSerotonin receptorsKi2.458.61PIGPDSP
5-HT1BSerotonin receptorsKi2.508.60HUMANPDSP
5-HT1BSerotonin receptorsKi2.508.60testPMID 28792478
5-HT2ASerotonin receptorsKi2.508.60RATPDSP
5-HT2CSerotonin receptorsKi2.508.60PIGPDSP
5-HT2CSerotonin receptorsKi2.518.60PIGPMID 10821800
5-HT2ASerotonin receptorsKi2.608.59RATPDSP
5-HT2ASerotonin receptorsKi2.698.57RATPDSP
5-HT2ASerotonin receptorsKi2.968.53RATPDSP
5-HT2ASerotonin receptorsKi3.058.52RATPDSP
5-HT2CSerotonin receptorsKi3.168.50PIGPDSP
5-HT2CSerotonin receptorsKi3.208.49PIGPDSP
5-HT2ASerotonin receptorsKi3.258.49HUMANPMID 16051647
5-HT2ASerotonin receptorsKi3.318.48HUMANPMID 7984267
5-HT1BSerotonin receptorsKi3.608.44HUMANPMID 1565658
5-HT1DSerotonin receptorsKi3.638.44HUMANPMID 7984267
5-HT1DSerotonin receptorsKi3.808.42COWPDSP
5-HT1DSerotonin receptorsKi3.808.42CALFPDSP
5-HT1DSerotonin receptorsKi3.808.42CALFPDSP
5-HT2ASerotonin receptorsKi3.838.42Homo sapiensCHEMBL1909211
5-HT1DSerotonin receptorsKi3.988.40CALFPDSP
5-HT2ASerotonin receptorsKi3.988.40HUMANPMID 7582481
5-HT2ASerotonin receptorsKi3.988.40HUMANPMID 7582481
5-HT2ASerotonin receptorsKi3.988.40HUMANPMID 15322733
5-HT1DSerotonin receptorsKi4.008.40BOVINEPMID 1565658
5-HT2CSerotonin receptorsKi4.478.35HUMANPMID 15322733
5-HT2Serotonin receptorsKi5.308.28Rattus norvegicusCHEMBL617424
5-HT2ASerotonin receptorsKi5.708.24RABBITPMID 9214741
5-HT2ASerotonin receptorsKi5.708.24HUMANPDSP
UncheckedUnclassifiedKi5.708.24— organism not recordedCHEMBL1007656
5-HT2BSerotonin receptorsKi6.288.20RATPMID 8632342
5-HT1FSerotonin receptorsKi6.308.20MOUSEPMID 7984267
5-HT2BSerotonin receptorsKi6.308.20RATPMID 7984267
5-HT2BSerotonin receptorsKi6.308.20RATPMID 7582481
5-HT2BSerotonin receptorsKi6.318.20RATPMID 10821800
5-HT2ASerotonin receptorsKi6.768.17RATPDSP
UncheckedUnclassifiedKi6.808.17— organism not recordedCHEMBL1013930
5-HT2ASerotonin receptorsKi7.008.15HUMANPDSP
5-HT1BSerotonin receptorsKi7.588.12HUMANPMID 7984267
5-HT2BSerotonin receptorsKi7.598.12Homo sapiensCHEMBL3106302
5-HT2BSerotonin receptorsKi7.608.12Homo sapiensCHEMBL3106302
5-HT1DSerotonin receptorsKi7.768.11DogPMID 7984267
5-HT2BSerotonin receptorsKi7.948.10HUMANPMID 7582481
5-HT2BSerotonin receptorsKi7.948.10HUMANPMID 10821800
5-HT1DSerotonin receptorsKi8.808.06BOVINEPMID 2664084
5-HT2BSerotonin receptorsKi9.108.04HUMANPMID 11104741
5-HT2ASerotonin receptorsKi9.808.01RATPDSP
5-HT7Serotonin receptorsKi12.507.90RATPMID 8394362
5-HT2BSerotonin receptorsKi12.587.90MOUSEPMID 7984267
5-HT6Serotonin receptorsKi12.587.90MOUSEPMID 8394987
5-HT7Serotonin receptorsKi12.587.90RATPMID 7984267
5-HT7Serotonin receptorsKi12.587.90MOUSEPMID 7984267
5-HT7Serotonin receptorsKi12.597.90RATPMID 9149537
5-HT7Serotonin receptorsKi12.597.90RATPMID 10821800
5-HT7Serotonin receptorsKi12.597.90Rattus norvegicusCHEMBL619052
5-HT7Serotonin receptorsKi12.597.90Homo sapiensCHEMBL619862
5-HT7Serotonin receptorsKi13.407.87RATPMID 8394362
5-HT1FSerotonin receptorsKi13.487.87RATPMID 7984267
5-HT7Serotonin receptorsKi13.487.87RATPMID 7984267
5-HT1ASerotonin receptorsKi14.007.85HUMANPDSP
5-HT1ASerotonin receptorsKi14.007.85testPMID 28792478
UncheckedUnclassifiedKi14.807.83— organism not recordedCHEMBL1013929
5-HT2ASerotonin receptorsKi15.007.82RATPDSP
5-HT2ASerotonin receptorsKi15.007.82RATPMID 11104741
5-HT1ASerotonin receptorsKi16.987.77HUMANPMID 7984267
5-HT7Serotonin receptorsKi17.007.77RATPMID 8398139
5-HT7Serotonin receptorsKi17.377.76RATPMID 7984267
5-HT2BSerotonin receptorsKi19.007.72HUMANPMID 24365264
5-HT7Serotonin receptorsKi19.957.70GUINEA PIGPMID 9149537
5-HT1ASerotonin receptorsKi21.207.67RATPDSP
5-HT7Serotonin receptorsKi22.387.65GUINEA PIGPMID 7647964
5-HT1ASerotonin receptorsKi23.447.63PIGPDSP
5-HT1ASerotonin receptorsKi24.207.62RATPDSP
5-HT1ASerotonin receptorsKi25.007.60HUMANPMID 16051647
5-HT1ASerotonin receptorsKi25.007.60RATPDSP
5-HT1ASerotonin receptorsKi25.007.60HUMANPMID 30768942
5-HT1DSerotonin receptorsKi25.007.60HUMANPMID 1565658
5-HT1BSerotonin receptorsKi25.117.60HUMANPMID 7984267
5-HT7Serotonin receptorsKi25.127.60HUMANPMID 9149537
5-HT2ASerotonin receptorsKi25.207.60HUMANPDSP
5-HT2ASerotonin receptorsKi26.307.58PIGPDSP
5-HT1DSerotonin receptorsKi26.907.57HUMANPDSP
5-HT7BSerotonin receptorsKi26.917.57HUMANPMID 9298538
5-HT6Serotonin receptorsKi30.007.52testPMID 28792478
5-HT7Serotonin receptorsKi30.007.52HUMANPDSP
5-HT1ASerotonin receptorsKi31.007.51Rattus norvegicusCHEMBL1909209
5-HT7Serotonin receptorsKi31.627.50RATPMID 9149537
5-HT1FSerotonin receptorsKi33.887.47HUMANPMID 7984267
5-HT1FSerotonin receptorsKi34.007.47HUMANPMID 8380639
5-HT7Serotonin receptorsKi39.817.40GUINEA PIGPMID 7518496
5-HT1ASerotonin receptorsKi40.007.40BOVINEPDSP
5-HT5BSerotonin receptorsKi40.707.39RATPMID 8224165
5-HT5BSerotonin receptorsKi40.737.39RATPMID 7984267
5-HT1DSerotonin receptorsKi41.007.39RATPDSP
5-HT2ASerotonin receptorsKi45.707.34HUMANPDSP
5-HT6Serotonin receptorsKi52.007.28HUMANPDSP
5-HT6Serotonin receptorsKi52.007.28testPMID 28792478
5-HT1ESerotonin receptorsKi59.007.23HUMANPMID 2664084
D3Dopamine receptorsKi59.007.23Homo sapiensCHEMBL1909141
5-HT5ASerotonin receptorsKi63.007.20MOUSEPMID 12825922
5-HT5ASerotonin receptorsKi63.097.20MOUSEPMID 7984267
5-HT5ASerotonin receptorsKi63.097.20MOUSEPMID 8450829
CB1Cannabinoid receptorsKi63.097.20MOUSEPMID 1464308
5-HT1DSerotonin receptorsKi69.007.16testPMID 28792478
5-HT1DSerotonin receptorsKi69.007.16HUMANPDSP
5-HT1ASerotonin receptorsKi70.797.15RATPMID 6225026
5-HT6Serotonin receptorsKi75.007.12Homo sapiensCHEMBL1909108
5-HT5ASerotonin receptorsKi79.437.10MOUSEPMID 7984267
5-HT7Serotonin receptorsKi79.437.10HUMANPMID 9149537
5-HT7Serotonin receptorsKi83.007.08HUMANPMID 12825922
5-HT7Serotonin receptorsKi83.007.08HUMANPMID 8226867
5-HT7Serotonin receptorsKi83.177.08HUMANPMID 7984267
5-HT2BSerotonin receptorsKi87.097.06RATPMID 7984267
Alpha2CAdrenergic receptorsKi88.307.05HUMANPDSP
5-HT1DSerotonin receptorsKi93.007.03HUMANPDSP
5-HT7Serotonin receptorsKi93.327.03GUINEA PIGPMID 7647964
5-HT1DSerotonin receptorsKi1007.00RATPDSP
5-HT2ASerotonin receptorsKi1046.98HUMANPDSP
Alpha2BAdrenergic receptorsKi1066.97HUMANPDSP
5-HT1BSerotonin receptorsKi1086.97Rattus norvegicusCHEMBL1909210
D2Dopamine receptorsKi1166.94RATPMID 6387355
5-HT1DSerotonin receptorsKi1206.92BOVINEPDSP
5-HT5BSerotonin receptorsKi1266.90MOUSEPMID 7984267
5-HT5BSerotonin receptorsKi1266.90MOUSEPMID 8450829
5-HT2BSerotonin receptorsKi1506.82HUMANPMID 12761331
D2Dopamine receptorsKi1606.80CALFPMID 995128
5-HT1BSerotonin receptorsKi1626.79HUMANPMID 7984267
Alpha2AAdrenergic receptorsKi1706.77HUMANPDSP
5-HT6Serotonin receptorsKi1806.74HUMANPMID 8522988
5-HT6Serotonin receptorsKi1806.74HUMANPMID 12825922
5-HT1BSerotonin receptorsKi1866.73GUINEA PIGPMID 11888550
5-HT5ASerotonin receptorsKi1956.71RATPMID 7984267
5-HT5BSerotonin receptorsKi1966.71RATPMID 7682702
D1Dopamine receptorsKi2176.66RATPMID 6387355
5-HT1ESerotonin receptorsKi2196.66HUMANPMID 7984267
5-HT1ESerotonin receptorsKi2286.64HUMANPMID 1513320
5-HT1ESerotonin receptorsKi2296.64HUMANPMID 7984267
5-HT1ESerotonin receptorsKi2376.63HUMANPDSP
5-HT1ESerotonin receptorsKi2376.63testPMID 28792478
5-HT6Serotonin receptorsKi2576.59RATPMID 9225298
D2Dopamine receptorsKi2696.57Homo sapiensCHEMBL1909140
D1Dopamine receptorsKi2906.54CALFPMID 995128
5-HT1ESerotonin receptorsKi3006.52RATPMID 8384716
5-HT1BSerotonin receptorsKi3096.51RATPMID 11888550
5-HT1ESerotonin receptorsKi3246.49HUMANPMID 7984267
5-HT6Serotonin receptorsKi3396.47RATPMID 9225298
5-HT6Serotonin receptorsKi3726.43RATPMID 7680751
5-HT6Serotonin receptorsKi3726.43HUMANPMID 8226867
5-HT1BSerotonin receptorsKi3866.41RATPMID 1738111
5-HT7Serotonin receptorsKi3986.40RATPMID 7984267
5-HT6Serotonin receptorsKi3986.40RATPMID 10821800
5-HT1BSerotonin receptorsKi4376.36RATPMID 7984267
D1Dopamine receptorsKi4726.33Homo sapiensCHEMBL1909139
5-HT5ASerotonin receptorsKi5006.30MOUSEPMID 8549774
5-HT1BSerotonin receptorsKi5206.28RATPDSP
5-HT1ASerotonin receptorsKi5456.26RATPMID 8398139
Alpha2AAdrenergic receptorsKi6116.21Homo sapiensCHEMBL1909088
5-HT5ASerotonin receptorsKi1,0006.00RATPMID 7682702
5-HT5BSerotonin receptorsKi1,0006.00RATPMID 7984267
5-HT1BSerotonin receptorsKi1,5105.82RATPDSP
D1Dopamine receptorsKi1,5825.80BOVINEPMID 2139469
UncheckedUnclassifiedKi1,6805.77— organism not recordedCHEMBL1909159
5-HT1BSerotonin receptorsKi1,8205.74RATPMID 7984267
Alpha2BAdrenergic receptorsKi2,1755.66Homo sapiensCHEMBL1909089
H1UnclassifiedKi3,0005.52HUMANPMID 16782354
H1UnclassifiedKi3,0005.52GUINEA PIGPDSP
UncheckedUnclassifiedKi3,1645.50— organism not recordedCHEMBL1909102
SERTMonoamine transportersKi3,7005.43RATPMID 2970277
M3UnclassifiedKi4,6325.33HUMANPDSP
5-HT1ASerotonin receptorsKi4,6775.33RATPMID 6225026
M1UnclassifiedKi5,4595.26HUMANPDSP
M2UnclassifiedKi6,1265.21HUMANPDSP
H1UnclassifiedKi9,0005.05HUMANPDSP

Functional readouts 14

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
5-HT2BSerotonin receptorsIC500.5639.25Homo sapiensCHEMBL1909104
5-HT2CSerotonin receptorsIC502.098.68Homo sapiensCHEMBL1909105
5-HT2ASerotonin receptorsIC5013.007.89Homo sapiensCHEMBL1909211
5-HT1ASerotonin receptorsIC5054.007.27Rattus norvegicusCHEMBL1909209
5-HT6Serotonin receptorsIC501626.79Homo sapiensCHEMBL1909108
D3Dopamine receptorsIC501726.76Homo sapiensCHEMBL1909141
5-HT1BSerotonin receptorsIC501776.75Rattus norvegicusCHEMBL1909210
D2Dopamine receptorsIC508076.09Homo sapiensCHEMBL1909140
Sigma 1Sigma receptorsIC509126.04Homo sapiensCHEMBL805753
D1Dopamine receptorsIC509436.03Homo sapiensCHEMBL1909139
Alpha2AAdrenergic receptorsIC501,6315.79Homo sapiensCHEMBL1909088
UncheckedUnclassifiedIC502,5195.60— organism not recordedCHEMBL1909159
UncheckedUnclassifiedIC503,5595.45— organism not recordedCHEMBL1909102
Alpha2BAdrenergic receptorsIC504,7635.32Homo sapiensCHEMBL1909089
P
PubChem
C
ChEMBL
R
Computed here with RDKit
D
Derived here from the stored measurement

IX · Trials

Registered clinical trials

Studies filed with ClinicalTrials.gov that name this compound as an intervention. A registered trial is a protocol, not a result — status and enrollment are printed beside every row, and withdrawn studies are counted rather than hidden.

— No registered study names Methysergide as an intervention. That is an absence of registered research, not evidence about the compound. Most of this archive has never been the subject of a registered trial.

Records from ClinicalTrials.gov (U.S. National Library of Medicine, NIH), API v2. A study is listed against a compound only when a verified name for that compound appears as a whole word in one of the study's own intervention names. A short code must appear as written, and a name the registry uses for something else (Aleph, a vaccine maker) is not matched. Title matches are not accepted. The matched name and the intervention text it matched are shown with every row.

Searched as Methysergide · Methysergid · 1-Methylmethylergonovine. Run this search at the registry.

A registered trial is a protocol somebody filed with the registry. It is not a result, and nothing on this plate says whether Methysergide worked.

XI · Literature

Sources behind this dossier

The papers this compound's values were read from, ranked by what each contributed. Not a review of the field.

Every paper below is one some value on this page came from — a binding constant, a passage of pharmacology or toxicology, or a measured duration. Each entry says what this archive took from it. Nothing else is claimed about any of them: the title is the study’s own account of itself, and a summary written here would be an assertion with no source behind it.

  1. 01

    Molecular biology of 5-HT receptors

    Boess FG, Martin IL · Neuropharmacology 1994

    • · 30 measurements at 10 targets (Ki), strongest 5-HT2A at 8.48 pX

    PMID 7984267

  2. 02

    Marine Inspired 2-(5-Halo-1H-indol-3-yl)-N,N-dimethylethanamines as Modulators of Serotonin Receptors: An Example Illustrating the Power of Bromine as Part of the Uniquely Marine Chemical Space

    Ibrahim MA, El-Alfy AT, Ezel K et al. · Marine drugs 2017

    • · 7 measurements at 6 targets (Ki), strongest 5-HT2B at 10.00 pX

    PMID 28792478

  3. 03

    The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors

    Bonhaus DW, Bach C, DeSouza A et al. · British journal of pharmacology 1995

    • · 7 measurements at 3 targets (Ki), strongest 5-HT2A at 8.80 pX

    PMID 7582481

  4. 04

    Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors

    Glusa E, Pertz HH · British journal of pharmacology 2000

    • · 5 measurements at 4 targets (Ki), strongest 5-HT2C at 8.60 pX

    PMID 10821800

  5. 05

    RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist

    Bonhaus DW, Weinhardt KK, Taylor M et al. · Neuropharmacology 1997

    • · 5 measurements at 3 targets (Ki), strongest 5-HT2C at 9.02 pX

    PMID 9225287

  6. 06

    The 5-HT7 receptor: orphan found

    Eglen RM, Jasper JR, Chang DJ et al. · Trends in pharmacological sciences 1997

    • · 5 measurements at 1 target (Ki), strongest 5-HT7 at 7.90 pX

    PMID 9149537

  7. 07

    Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors

    Knight AR, Misra A, Quirk K et al. · Naunyn-Schmiedeberg's archives of pharmacology 2004

    • · 3 measurements at 3 targets (Ki), strongest 5-HT2B at 9.44 pX

    PMID 15322733

  8. 08

    Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7)

    Glennon RA · Journal of medicinal chemistry 2003

    • · 3 measurements at 3 targets (Ki), strongest 5-HT5A at 7.20 pX

    PMID 12825922

  9. 09

    Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications

    Rothman RB, Baumann MH, Savage JE et al. · Circulation 2000

    • · 3 measurements at 3 targets (Ki), strongest 5-HT2C at 8.74 pX

    PMID 11104741

  10. 10

    Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta

    Weinshank RL, Zgombick JM, Macchi MJ et al. · Proceedings of the National Academy of Sciences of the United States of America 1992

    • · 3 measurements at 2 targets (Ki), strongest 5-HT1B at 8.44 pX

    PMID 1565658

  11. 11

    Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity

    Gillman PK · British journal of anaesthesia 2005

    • · 2 measurements at 2 targets (Ki), strongest 5-HT2A at 8.49 pX

    PMID 16051647

  12. 12

    Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization

    Millan MJ, Newman-Tancredi A, Lochon S et al. · Pharmacology, biochemistry, and behavior 2002

    • · 2 measurements at 1 target (Ki), strongest 5-HT1B at 6.73 pX

    PMID 11888550

  13. 13

    Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors

    Egan C, Grinde E, Dupre A et al. · Synapse (New York, N.Y.) 2000

    • · 2 measurements at 1 target (Ki), strongest 5-HT2C at 9.10 pX

    PMID 10611640

  14. 14

    [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor

    Wainscott DB, Sasso DA, Kursar JD et al. · Naunyn-Schmiedeberg's archives of pharmacology 1998

    • · 2 measurements at 1 target (Ki), strongest 5-HT2B at 9.19 pX

    PMID 9459568

  15. 15

    Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor

    Herrick-Davis K, Grinde E, Gauthier C et al. · Annals of the New York Academy of Sciences 1998

    • · 2 measurements at 1 target (Ki), strongest 5-HT2C at 9.10 pX

    PMID 9928251

  16. 16

    Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells

    Boess FG, Monsma FJ Jr, Carolo C et al. · Neuropharmacology 1997

    • · 2 measurements at 1 target (Ki), strongest 5-HT6 at 6.59 pX

    PMID 9225298

  17. 17

    Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences

    Wainscott DB, Lucaites VL, Kursar JD et al. · The Journal of pharmacology and experimental therapeutics 1996

    • · 2 measurements at 1 target (Ki), strongest 5-HT2B at 8.80 pX

    PMID 8632342

  18. 18

    Characterization and distribution of putative 5-ht7 receptors in guinea-pig brain

    To ZP, Bonhaus DW, Eglen RM et al. · British journal of pharmacology 1995

    • · 2 measurements at 1 target (Ki), strongest 5-HT7 at 7.65 pX

    PMID 7647964

  19. 19

    A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms

    Lovenberg TW, Baron BM, de Lecea L et al. · Neuron 1993

    • · 2 measurements at 2 targets (Ki), strongest 5-HT7 at 7.77 pX

    PMID 8398139

  20. 20

    Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase

    Bard JA, Zgombick J, Adham N et al. · The Journal of biological chemistry 1993

    • · 2 measurements at 2 targets (Ki), strongest 5-HT7 at 7.08 pX

    PMID 8226867

  21. 21

    Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype

    Shen Y, Monsma FJ Jr, Metcalf MA et al. · The Journal of biological chemistry 1993

    • · 2 measurements at 1 target (Ki), strongest 5-HT7 at 7.90 pX

    PMID 8394362

  22. 22

    Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization

    Matthes H, Boschert U, Amlaiky N et al. · Molecular pharmacology 1993

    • · 2 measurements at 2 targets (Ki), strongest 5-HT5A at 7.20 pX

    PMID 8450829

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    Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain

    Erlander MG, Lovenberg TW, Baron BM et al. · Proceedings of the National Academy of Sciences of the United States of America 1993

    • · 2 measurements at 2 targets (Ki), strongest 5-HT5B at 6.71 pX

    PMID 7682702

  24. 24

    Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein

    Leonhardt S, Herrick-Davis K, Titeler M · Journal of neurochemistry 1989

    • · 2 measurements at 2 targets (Ki), strongest 5-HT1D at 8.06 pX

    PMID 2664084

  25. 25

    Characterization of the binding of 3H-SCH 23390, a selective D-1 receptor antagonist ligand, in rat striatum

    Billard W, Ruperto V, Crosby G et al. · Life sciences 1984

    • · 2 measurements at 2 targets (Ki), strongest D2 at 6.94 pX

    PMID 6387355

  26. 26

    Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT

    Gozlan H, El Mestikawy S, Pichat L et al. · Nature 1983

    • · 2 measurements at 1 target (Ki), strongest 5-HT1A at 7.15 pX

    PMID 6225026

  27. 27

    Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes

    Burt DR, Creese I, Snyder SH · Molecular pharmacology 1976

    • · 2 measurements at 2 targets (Ki), strongest D2 at 6.80 pX

    PMID 995128

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    Evaluation of SYA16263 as a new potential antipsychotic agent without catalepsy

    Bricker BA, Peprah K, Kang HJ et al. · Pharmacology, biochemistry, and behavior 2019

    • · 1 measurement at 1 target (Ki), strongest 5-HT1A at 7.60 pX

    PMID 30768942

  29. 29

    Molecular interactions between general anesthetics and the 5HT2B receptor

    Matsunaga F, Gao L, Huang XP et al. · Journal of biomolecular structure & dynamics 2015

    • · 1 measurement at 1 target (Ki), strongest 5-HT2B at 7.72 pX

    PMID 24365264

  30. 30

    Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands

    Furlotti G, Alisi MA, Apicella C et al. · Journal of medicinal chemistry 2012

    • · 1 measurement at 1 target (Ki), strongest 5-HT2A at 8.80 pX

    PMID 23043420

  31. 31

    Novel ligands for the human histamine H1 receptor: synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1,2,3,4-tetrahydronaphthalenes

    Ghoneim OM, Legere JA, Golbraikh A et al. · Bioorganic & medicinal chemistry 2006

    • · 1 measurement at 1 target (Ki), strongest H1 at 5.52 pX

    PMID 16782354

  32. 32

    3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro

    Setola V, Hufeisen SJ, Grande-Allen KJ et al. · Molecular pharmacology 2003

    • · 1 measurement at 1 target (Ki), strongest 5-HT2B at 6.82 pX

    PMID 12761331

  33. 33

    Activity of Parthenolide at 5HT2A receptors

    Weber JT, O'Connor MF, Hayataka K et al. · Journal of natural products 1997

    • · 1 measurement at 1 target (Ki), strongest 5-HT2A at 8.24 pX

    PMID 9214741

  34. 34

    Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b)

    Jasper JR, Kosaka A, To ZP et al. · British journal of pharmacology 1997

    • · 1 measurement at 1 target (Ki), strongest 5-HT7B at 7.57 pX

    PMID 9298538

  35. 35

    Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor

    Kohen R, Metcalf MA, Khan N et al. · Journal of neurochemistry 1996

    • · 1 measurement at 1 target (Ki), strongest 5-HT6 at 6.74 pX

    PMID 8522988

  36. 36

    Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding

    Schotte A, Janssen PF, Gommeren W et al. · Psychopharmacology 1996

    • · 1 measurement at 1 target (Ki), strongest 5-HT2A at 9.38 pX

    PMID 8935801

  37. 37

    BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex

    Borsini F, Giraldo E, Monferini E et al. · Naunyn-Schmiedeberg's archives of pharmacology 1995

    • · 1 measurement at 1 target (Ki), strongest 5-HT2A at 8.89 pX

    PMID 8584042

  38. 38

    Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization

    Weiss HM, Haase W, Michel H et al. · FEBS letters 1995

    • · 1 measurement at 1 target (Ki), strongest 5-HT5A at 6.30 pX

    PMID 8549774

  39. 39

    Cloning and expression of a 5-hydroxytryptamine7 receptor positively coupled to adenylyl cyclase

    Tsou AP, Kosaka A, Bach C et al. · Journal of neurochemistry 1994

    • · 1 measurement at 1 target (Ki), strongest 5-HT7 at 7.40 pX

    PMID 7518496

  40. 40

    Cloning and characterization of the rat 5-HT5B receptor. Evidence that the 5-HT5B receptor couples to a G protein in mammalian cell membranes

    Wisden W, Parker EM, Mahle CD et al. · FEBS letters 1993

    • · 1 measurement at 1 target (Ki), strongest 5-HT5B at 7.39 pX

    PMID 8224165

  41. 41

    Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs

    Monsma FJ Jr, Shen Y, Ward RP et al. · Molecular pharmacology 1993

    • · 1 measurement at 1 target (Ki), strongest 5-HT6 at 6.43 pX

    PMID 7680751

  42. 42

    Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase

    Adham N, Kao HT, Schecter LE et al. · Proceedings of the National Academy of Sciences of the United States of America 1993

    • · 1 measurement at 1 target (Ki), strongest 5-HT1F at 7.47 pX

    PMID 8380639

  43. 43

    Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes

    Lovenberg TW, Erlander MG, Baron BM et al. · Proceedings of the National Academy of Sciences of the United States of America 1993

    • · 1 measurement at 1 target (Ki), strongest 5-HT1E at 6.52 pX

    PMID 8384716

  44. 44

    Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase

    Plassat JL, Amlaiky N, Hen R · Molecular pharmacology 1993

    • · 1 measurement at 1 target (Ki), strongest 5-HT6 at 7.90 pX

    PMID 8394987

  45. 45

    Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release

    Matsumoto I, Combs MR, Jones DJ · The Journal of pharmacology and experimental therapeutics 1992

    • · 1 measurement at 1 target (Ki), strongest 5-HT1B at 6.41 pX

    PMID 1738111

  46. 46

    Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor

    Zgombick JM, Schechter LE, Macchi M et al. · Molecular pharmacology 1992

    • · 1 measurement at 1 target (Ki), strongest 5-HT1E at 6.64 pX

    PMID 1513320

  47. 47

    The mouse 5HT5 receptor reveals a remarkable heterogeneity within the 5HT1D receptor family

    Plassat JL, Boschert U, Amlaiky N et al. · The EMBO journal 1992

    • · 1 measurement at 1 target (Ki), strongest CB1 at 7.20 pX

    PMID 1464308

  48. 48

    Characterization of D1 dopamine receptors in the bovine pineal gland with [3H]SCH 23390

    Simonneaux V, Murrin LC, Ebadi M · The Journal of pharmacology and experimental therapeutics 1990

    • · 1 measurement at 1 target (Ki), strongest D1 at 5.80 pX

    PMID 2139469

  49. 49

    Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine

    Kovachich GB, Aronson CE, Brunswick DJ et al. · Brain research 1988

    • · 1 measurement at 1 target (Ki), strongest SERT at 5.43 pX

    PMID 2970277

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    [Chronic ergotism: spinal lesion and neuropathy]

    Sallansonnet-Froment M, Guegan-Massardier E, Blohorn-Sense A et al. · Revue neurologique 2004

    • · Human Toxicity Excerpts

    PMID 15454875

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    Antinociceptive effects of methysergide in various pain models

    Chung KM, Choi SS, Han KJ et al. · Pharmacology 2003

    • · Mechanism of Action

    PMID 12928583

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    Methysergide-induced retroperitoneal fibrosis: successful outcome and two new laboratory features

    Bucci JA, Manoharan A · Mayo Clinic proceedings 1997

    • · Human Toxicity Excerpts

    PMID 9413296

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    Pharmacokinetics of methysergide and its metabolite methylergometrine in man

    Bredberg U, Eyjolfsdottir GS, Paalzow L et al. · European journal of clinical pharmacology 1986

    • · Biological Half-Life

    PMID 3709634

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    Effect of two antiserotoninergic drugs, methysergide and metergoline, on gastric acid secretion and gastrin release in healthy man

    Caldara R, Ferrari C, Barbieri C et al. · European journal of clinical pharmacology 1980

    • · Human Toxicity Excerpts

    PMID 7371695