Tiletamine
Also known asTiletamina · Tiletaminum · Tiletamine (INN) · TILETAMINE [INN] · Tiletaminum [INN-Latin] · Tiletamina [INN-Spanish] · TILETAMINE [MI] · TILETAMINE [WHO-DD]
2-(ethylamino)-2-thiophen-2-ylcyclohexan-1-one
- PubChem CID
- 26533
- ChEMBL
- CHEMBL1474801
- Measurements
- 0
- InChIKey
- QAXBVGVYDCAVLV-UHFFFAOYSA-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
2-(ethylamino)-2-thiophen-2-yl-1-cyclohexanone is an aralkylamine.
This drug is a dissociative anesthetic agent that falls under the drug category of NMDA receptor antagonists. Tiletamine is chemically similar to another dissociative anesthetic, ketamine. Tiletamine hydrochloride, the salt form, exists as odorless white crystals.
Proposed anesthetic with possible anticonvulsant and sedative properties.
See also: Lidocaine Hydrochloride (related); Ketamine (related); Tiletamine Hydrochloride (active moiety of).
Recognized use
/VET/ This study is the first to compare the anesthetic effects of two cyclohexamines on free-ranging subantarctic fur seal (Arctocephalus tropicalis) females. From April to July 1999, 107 females were immobilized for tooth extraction and blood sampling, using either ketamine (Ketalar, n = 58) alone or tiletamine-zolazepam (Zoletil 100, n = 49) mixture. Animals were injected intramuscularly at mean doses of 2.1 mg/kg for ketamine and 1.1 mg/kg for tiletamine-zolazepam mixture. Individual response to both drugs was highly variable. The dosage required to achieve a satisfactory level of anesthesia was smaller for subantarctic fur seals than for most other species of seals and was less for anim…
Therapeutic Uses
Hazardous Substances Data Bank (HSDB)PMID 12528456Dabin W et al; J Wildl Dis 38 (4): 846-50 (2002)
Telazol; /mixture of/ Tiletamine HCl & Zolazapam HCl /is a/ veterinary pharmaceutical /used as a/ general anesthetic. /Telazol/
Therapeutic Uses
Hazardous Substances Data Bank (HSDB)Fort Dodge; Material Safety Data Sheet (MSDS) on Telazol p.1 (2002) Available from https://www.accessbutler.com/msdsimages/A0000865.pdf as of November 19, 2008
/VET/ Intramuscular injection of tiletamine-zolazepam and xylazine is commonly used as a preanesthetic for veterinary surgical procedures and for short-term restraint. However, this combination can have marked cardiodepressive and hypothermic effects that persist for hours to days. Here ... a case report of these effects in a swine heart failure model /is presented/.
Therapeutic Uses
Hazardous Substances Data Bank (HSDB)PMID 17994676Lefkov SH, Mussig D; J Am Assoc Lab Anim Sci 46 (6): 63-4 (2007)
/VET/ Medetomidine (0.02-0.06 mg/kg) in combination with zolazepam-tiletamine (0.8-2.3 mg/kg) were evaluated for reversible anesthesia in four species of Southeast Asian primates: Bornean orangutan (Pongo pygmaeus pygmaeus), Bornean gibbon (Hylobates muelleri), long-tailed macaque (Macaca fascicularis), and pig-tailed macaque (Macaca nemestrina). Twenty-three anesthetic procedures of captive-held and free-ranging primates were studied in Sabah, Malaysia. The induction was smooth and rapid. Respiratory and heart rates were stable throughout anesthesia, whereas body temperature and systolic arterial blood pressure decreased significantly. Atipamezole at five times the medetomidine dose effecti…
Therapeutic Uses
Hazardous Substances Data Bank (HSDB)PMID 17315446Fahlman A et al; J Zoo Wildl Med 37 (4): 558-61
... rapid-acting, nonnarcotic, nonbarbituate drug used to produce anesthesia in cats and dogs
Use Classification
Hazardous Substances Data Bank (HSDB)Sams R; Ullmann's Encyclopedia of Industrial Chemistry. 7th ed. (2008). NY, NY: John Wiley & Sons; Veterinary Drugs. Online Posting Date: Jun 15, 2000.
How it acts
Neurochemical interactions of tiletamine, a potent phencyclidine (PCP) receptor ligand, with the N-methyl-D-aspartate (NMDA)-coupled and -uncoupled PCP recognition sites were examined. Tiletamine potently displaced the binding of [3H]1-(2-thienyl)cyclohexylpiperidine with an IC50 of 79 nM without affecting sigma-, glycine, glutamate, kainate, quisqualate, or dopamine (DA) receptors. Like other PCP ligands acting via the NMDA-coupled PCP recognition sites, tiletamine decreased basal, harmaline-, and D-serine-mediated increases in cyclic GMP levels and induced stereotypy and ataxia. Tiletamine was nearly five times more potent than PCP at inhibiting the binding of 3-hydroxy[3H]PCP to its high-…
Hazardous Substances Data Bank (HSDB)PMID 1847186Rao TS et al; J Neurochem 56 (3): 890-7 (1991)
...This study shows tiletamine to be similar to ketamine and to phencyclidine, agents known to interact with the N-methyl-D,L-aspartate (NMA) receptor. Effects of tiletamine on synaptic transmission and on direct excitatory responses to exogenous amino acids were examined in rat hippocampal and striatal slices. In striatal slices, tiletamine inhibited the NMA-mediated, but not the spontaneous, release of [3H]acetylcholine, with an IC50 of 70 nM. In hippocampal CA1 cells, 3 uM tiletamine in the perfusate reversibly blocked the intracellularly recorded responses to ionophoretically applied NMA, but not to glutamate, quisqualate and kainate. Tiletamine, 3 to 100 uM, had no effect on the orthodr…
Hazardous Substances Data Bank (HSDB)PMID 3320347French-Mullen JM et al; J Pharmacol Exp Ther 243 (3): 915-20 (1987)
Behavior carries the pharmacological classes and the acute-effect durations, with plasma half-life kept separate from duration of effect.
In the body
A pharmacokinetic and tissue residue study was conducted to assess the risks associated with human consumption of polar bears in arctic Canada that have been exposed to the immobilizing drug Telazol, a mixture of tiletamine hydrochloride and zolazepam hydrochloride. Twenty-two bears were remotely injected with about 10 mg/kg of Telazol. Following immobilization, serum samples were collected serially at regular intervals until the bears awakened. Sixteen of the bears were relocated and killed under permit by local hunters at various times from 0.5 to 11 days after dosing. Serum, kidney, muscle and adipose tissue samples were collected immediately after death. ... In addition, the serum and ti…
Hazardous Substances Data Bank (HSDB)PMID 11085426Semple HA et al; J Wildl Dis 36 (4): 653-62 (2000)
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 Tiletamine 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 Tiletamine 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.
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.
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
- Toxicology — 5 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.
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 Tiletamine 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.
- Formula
- C12H17NOSR
- Molecular weight
- 223.34g/molR
- Exact mass
- 223.1031DaR
- cLogP
- 2.70R
- TPSA
- 29.1ŲR
- H-bond donors
- 1R
- H-bond acceptors
- 3R
- Rotatable bonds
- 3R
- Aromatic rings
- 1R
- Heavy atoms
- 15R
- Fraction sp³
- 0.583R
- Formal charge
- 0R
Computed with RDKit 2025.09.2 from the SMILES returned by PubChem. Audit run 26/09/2026.
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.
No half-life is published for this compound in the sources this site reads.
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.
Neurochemical interactions of tiletamine, a potent phencyclidine (PCP) receptor ligand, with the N-methyl-D-aspartate (NMDA)-coupled and -uncoupled PCP recognition sites were examined. Tiletamine potently displaced the binding of [3H]1-(2-thienyl)cyclohexylpiperidine with an IC50 of 79 nM without affecting sigma-, glycine, glutamate, kain…
Hazardous Substances Data Bank (HSDB)PMID 1847186Rao TS et al; J Neurochem 56 (3): 890-7 (1991) ...This study shows tiletamine to be similar to ketamine and to phencyclidine, agents known to interact with the N-methyl-D,L-aspartate (NMA) receptor. Effects of tiletamine on synaptic transmission and on direct excitatory responses to exogenous amino acids were examined in rat hippocampal and striatal slices. In striatal slices, tiletam…
Hazardous Substances Data Bank (HSDB)PMID 3320347French-Mullen JM et al; J Pharmacol Exp Ther 243 (3): 915-20 (1987)
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.
Filed under Anesthetics, Dissociative
- 6C4DDisorders due to use of dissociative drugs including ketamine and phencyclidine [PCP]
Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, Text Revision (DSM-5-TR): Phencyclidine-Related Disorders. Category names only — the manual is in copyright and no diagnostic criterion is reproduced here.
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.
- Cognition 2
- matched on “concentrat” · in PMID 10517567; PMID 10872580
VI · Profile
Affinity rosette
No measurement for Tiletamine converts to an affinity at a molecular target, so there is no rosette to draw. This is an absence of data, not a finding about the compound.
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 Tiletamine in this archive.
As published
Quoted verbatim from the database named after each passage, never summarized — a summary of a toxicology statement is a new claim.
Human Toxicity Excerpts
/SIGNS AND SYMPTOMS/ Potential organ systems affected are: Central Nervous System. Adverse effects could include: dizziness, light headedness, headache, nausea, and blurred vision. /Telazol/
Hazardous Substances Data Bank (HSDB)Fort Dodge; Material Safety Data Sheet (MSDS) on Telazol p.1 (2002) Available from https://www.accessbutler.com/msdsimages/A0000865.pdf as of November 19, 2008
/SIGNS AND SYMPTOMS/ Telazol causes almost immediate anesthetic effects, and sudden alertness is not uncommon as the effects of the drug subside. /Telazol/
Hazardous Substances Data Bank (HSDB)PMID 11527235Quail MT et al; J Toxicol Clin Toxicol 39 (4): 399-402 (2001)
/CASE REPORTS/ A 45-year-old male veterinarian was found dead in bed. Police investigation showed no evidence of trauma or other suspicious circumstances. Autopsy was unremarkable except for cardiomegaly and hepatosplenomegaly. Toxicological analysis revealed the presence of Telazol and ketamine. Telazol is a veterinary anesthetic agent that is composed of equal parts of tiletamine and zolazepam. Tiletamine is a disa…
Hazardous Substances Data Bank (HSDB)PMID 10517567Cording CJ et al; J Anal Toxicol 23 (6): 552-5 (1999)
/CASE REPORTS/ A 22-year-old male with more than 28 needle marks on his right arm was found dead. First, he was suspected as a drug abuser. Blood, urine, spleen, and injection-site tissue was collected during autopsy. The blood and urine specimens were screened for drugs. Immunoassay studies did not show any illegal drugs. However, two unidentified peaks were isolated in both of these biological fluids by routine gas…
Hazardous Substances Data Bank (HSDB)PMID 10872580Chung H et al; J Anal Toxicol 24 (4): 305-8 (2000)
/CASE REPORTS/ A 30-year-old female employee at a local zoo was found unresponsive by fellow workers in a clean animal treatment room. Initial reports were that she had injected veterinary-grade diazepam and telazol. On-scene paramedics reported her as obtunded and arousable to deep painful stimuli, with gag reflex intact. Systolic blood pressure was 90 mm Hg by palpation. A fresh needle puncture mark was present on…
Hazardous Substances Data Bank (HSDB)PMID 11527235Quail MT et al; J Toxicol Clin Toxicol 39 (4): 399-402 (2001)
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.
No bioactivity measurement is recorded for this compound in the archive.
- 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 Tiletamine 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 Tiletamine · Tiletamina · Tiletaminum. 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 Tiletamine worked.
X · Legal
Controlled-substance status
United States federal scheduling, read from the DEA records this archive holds. Not legal advice, and an absent record is not a finding that a compound is uncontrolled.
Other regulatory records
Registers outside the DEA that hold an entry for Tiletamine — chemical-safety and national inventories, each naming itself. They are not scheduling decisions.
Tiletamine hydrochloride and zolazepam hydrochloride for injection. ... Indications for use. It is used for restraint or for anesthesia combined with muscle relaxation in cats and in dogs for restraint and minor procedures of short duration (30 minutes) requiring mild to moderate analgesia. ... Limitations. Discard unused reconstituted solution after 48 hours. Not for use in dogs and cats with pancreatic disease, or with severe cardiac or pulmonary dysfunction. Not for use in pregnant animals. Not for use in cats suffering with renal insufficiency. The dosage should be reduced in geriatric dogs and cats. Federal law restricts this drug to use by or on the order of a licensed veterinarian. /T…
Hazardous Substances Data Bank (HSDB)21 CFR 522.2470 (USFDA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of November 21, 2008: https://www.ecfr.gov
Schedule III shall consist of the drugs and other substances, by whatever official name, common or usual name, chemical name, or brand name designated, listed in this section. Each drug or substance has been assigned the DEA Controlled Substances Code Number set forth opposite it. ... Unless specifically excepted or unless listed in another schedule, any material, compound, mixture, or preparation which contains any quantity of the following substances having a depressant effect on the central nervous system: Tiletamine and zolazepam or any salt thereof. DEA Code Number: 7295.
Hazardous Substances Data Bank (HSDB)21 CFR 1308.13(c) (USDEA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of November 17, 2008: https://www.ecfr.gov
An absent DEA record is not a finding that Tiletamine is legal. It means this archive holds no DEA passage for it. The Controlled Substances Analogue Enforcement Act reaches substances that appear on no schedule by name, and many compounds here are ring-substituted analogues of scheduled drugs. Nothing on this plate should be read as saying a compound may lawfully be made, held or supplied.
United States federal status only. State law differs, and so does the law of every other country — none of it is represented here. Scheduling changes, and this reflects the DEA records held by PubChem descriptive sections when the monograph was last harvested, not necessarily today. This is a record of what a database publishes, not legal advice.
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.
- 01
Abuse of telazol: an animal tranquilizer
Quail MT, Weimersheimer P, Woolf AD et al. · Journal of toxicology. Clinical toxicology 2001
- · Human Toxicity Excerpts
- 02
A fatality due to injection of tiletamine and zolazepam
Chung H, Choi H, Kim E et al. · Journal of analytical toxicology 2000
- · Human Toxicity Excerpts
- 03
A fatality related to the veterinary anesthetic telazol
Cording CJ, DeLuca R, Camporese T et al. · Journal of analytical toxicology 1999
- · Human Toxicity Excerpts
- 04
Rao TS, Contreras PC, Cler JA et al. · Journal of neurochemistry 1991
- · Mechanism of Action
- 05
ffRench-Mullen JM, Lehmann J, Bohacek R et al. · The Journal of pharmacology and experimental therapeutics 1987
- · Mechanism of Action