Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C12H17NOS |
| Molecular Weight | 223.334 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCNC1(CCCCC1=O)C2=CC=CS2
InChI
InChIKey=QAXBVGVYDCAVLV-UHFFFAOYSA-N
InChI=1S/C12H17NOS/c1-2-13-12(11-7-5-9-15-11)8-4-3-6-10(12)14/h5,7,9,13H,2-4,6,8H2,1H3
| Molecular Formula | C12H17NOS |
| Molecular Weight | 223.334 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
Tiletamine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist chemically related to ketamine and phencyclidine. A common veterinary anesthetic drug, tiletamine is currently a Schedule III controlled substance in USA. This compound exerts sedative effects in humans and animals, also having an abuse potential, toxicity and dissociative hallucinogenic properties clinically. In combination with benzodiazepine, zolazepam it is used as veterinary drug, called as telazol. Telazol is a nonnarcotic, nonbarbiturate, injectable anesthetic agent, which is indicated in cats for restraint or for anesthesia combined with muscle relaxation and in dogs for restraint and minor procedures of short duration (30 min) requiring mild to moderate analgesia. Tiletamine exerts sedative effects in humans and animals, also having an abuse potential, toxicity and dissociative hallucinogenic properties clinically.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28343145
Curator's Comment: Known to be CNS penetrant in rat. Human data not available
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3442 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2846121 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | TELAZOL Approved UseUnknown |
Doses
| Dose | Population | Adverse events |
|---|---|---|
30 mg 6 times / day multiple, intravenous Abused dose Dose: 30 mg, 6 times / day Route: intravenous Route: multiple Dose: 30 mg, 6 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
Disc. AE: Auditory hallucinations, Persecutory delusion... AEs leading to discontinuation/dose reduction: Auditory hallucinations Sources: Persecutory delusion Dissociative states Psychosis |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Auditory hallucinations | Disc. AE | 30 mg 6 times / day multiple, intravenous Abused dose Dose: 30 mg, 6 times / day Route: intravenous Route: multiple Dose: 30 mg, 6 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Dissociative states | Disc. AE | 30 mg 6 times / day multiple, intravenous Abused dose Dose: 30 mg, 6 times / day Route: intravenous Route: multiple Dose: 30 mg, 6 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Persecutory delusion | Disc. AE | 30 mg 6 times / day multiple, intravenous Abused dose Dose: 30 mg, 6 times / day Route: intravenous Route: multiple Dose: 30 mg, 6 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Psychosis | Disc. AE | 30 mg 6 times / day multiple, intravenous Abused dose Dose: 30 mg, 6 times / day Route: intravenous Route: multiple Dose: 30 mg, 6 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Transcriptomic analysis of the venom gland of the red-headed krait (Bungarus flaviceps) using expressed sequence tags. | 2010-03-29 |
|
| Dorsal arthrodesis in prepubertal New Zealand white rabbits followed to skeletal maturity: Effect on thoracic dimensions, spine growth and neural elements. | 2010-01 |
|
| Use of hyaluronidase to improve chemical immobilization of free-ranging polar bears (Ursus maritimus). | 2010-01 |
|
| Evaluation of anesthetic protocol for the collection of semen from captive collared peccaries (Tayassu tajacu) by electroejaculation. | 2009-12 |
|
| Effects of different general anesthetics on serum hemolysis and hepatic and muscular glycogenolysis in rats. | 2009-11 |
|
| The effect of amnion-derived cellular cytokine solution on the epithelialization of partial-thickness donor site wounds in normal and streptozotocin-induced diabetic swine. | 2009-10-20 |
|
| Movement disorder caused by abuse of veterinary anesthesia containing tiletamine. | 2009-10 |
|
| A serological survey of infectious disease in Yellowstone National Park's canid community. | 2009-09-16 |
|
| Efficacy of strain RB51 vaccine in protecting infection and vertical transmission against Brucella abortus in Sprague-Dawley rats. | 2009-09 |
|
| Evaluation of three immobilization combinations in the capybara (Hydrochoerus hydrochaeris). | 2009-08-01 |
|
| In vivo properties of the proangiogenic peptide QK. | 2009-06-08 |
|
| The effects of different anesthetic agents on short electroretinography protocol in dogs. | 2009-06 |
|
| Use of two anesthetic combinations for semen collection by electroejaculation from captive coatis (Nasua nasua). | 2009-05 |
|
| A pig model of acute Staphylococcus aureus induced pyemia. | 2009-03-27 |
|
| Comparison of azaperone-detomidine-butorphanol-ketamine and azaperone-tiletamine-zolazepam for anaesthesia in piglets. | 2009-03 |
|
| Biliary clearance of bromosulfophthalein in anesthetized and freely moving conscious rat. | 2009-03 |
|
| Urinary cortisol responses to unusual events in captive chimpanzees (Pan troglodytes). | 2009-01 |
|
| Insulin reduces cerebral ischemia/reperfusion injury in the hippocampus of diabetic rats: a role for glycogen synthase kinase-3beta. | 2009-01 |
|
| Acute effects of an alternative electronic-control-device waveform in swine. | 2009 |
|
| Reversible immobilization of asiatic black bear (Ursus thibetanus) with detomidine-tiletamine-zolazepam and atipamezole. | 2008-12 |
|
| Effects of premedication with tiletamine/zolazepam/medetomidine during general anesthesia using sevoflurane/fentanyl in swine undergoing pancreas transplantation. | 2008-11 |
|
| Methods of advanced wound management for care of combined traumatic and chemical warfare injuries. | 2008-07-21 |
|
| Principal component analysis for the comparison of metabolic profiles from human rectal cancer biopsies and colorectal xenografts using high-resolution magic angle spinning 1H magnetic resonance spectroscopy. | 2008-04-25 |
|
| Biomedical evaluation of free-ranging red ruffed lemurs (Varecia rubra) within the Masoala National Park, Madagascar. | 2008-03 |
|
| Clinical and pathologic features of cynomolgus macaques (Macaca fascicularis) infected with aerosolized Yersinia pestis. | 2008-02 |
|
| Effects of acepromazine and butorphanol on tiletamine-zolazepam anesthesia in llamas. | 2008-02 |
|
| Effects of two different anaesthetics on serum concentrations of cortisol and luteinizing hormone in barrows and gilts. | 2008-01 |
|
| Changes in minimal alveolar concentration of isoflurane following treatment with medetomidine and tiletamine/zolazepam, epidural morphine or systemic buprenorphine in pigs. | 2008-01 |
|
| Echocardiographic reference ranges for sedated healthy cynomolgus monkeys (Macaca fascicularis). | 2008-01 |
|
| Antagonistic effects of yohimbine in pigs anaesthetised with tiletamine/zolazepam and xylazine. | 2007-11-03 |
|
| Tiletamine-zolazepam and xylazine is a potent cardiodepressive combination: a case report. | 2007-11 |
|
| Nitric oxide and angiotensin II receptors mediate the pressor effect of angiotensin II: a study in conscious and zoletil-anesthetized rats. | 2007-11 |
|
| Performance measurements in endolaparoscopic infrarenal aortic graft implantation using computer-enhanced instrumentation: a laboratory model for training. | 2007-10-13 |
|
| Pseudomyxoma peritonei--two novel orthotopic mouse models portray the PMCA-I histopathologic subtype. | 2007-06-30 |
|
| Effects of tiletamine-zolazepam anaesthesia on plasma antioxidative status and some haematological parameters in sheep. | 2007-06 |
|
| Tiletamine-zolazepam-xylazine immobilization of fishers (Martes pennanti). | 2007-04 |
|
| Immobilization of Japanese black bears (Ursus thibetanus japonicus) with tiletamine hydrochloride and zolazepam hydrochloride. | 2007-04 |
|
| Comparison of cardiovascular effects of tiletamine-zolazepam, pentobarbital, and ketamine-xylazine in male rats. | 2007-03 |
|
| A comparison of anesthetic and cardiorespiratory effects of tiletamine-zolazepam-butorphanol and tiletamine-zolazepam-butorphanol- medetomidine in cats. | 2007 |
|
| Comparison of anesthetic and cardiorespiratory effects of tiletamine-zolazepam-butorphanol and tiletamine-zolazepam-butorphanol-medetomidine in dogs. | 2007 |
|
| Cardiopulmonary effects of medetomidine or midazolam in combination with ketamine or tiletamine/zolazepam for the immobilisation of captive cheetahs (Acinonyx jubatus). | 2006-12 |
|
| Reversible anesthesia of Southeast Asian primates with medetomidine, zolazepam, and tiletamine. | 2006-12 |
|
| Pharmacokinetics of tiletamine and zolazepam (Telazol) in anesthetized pigs. | 2006-12 |
|
| Determination of constituents of Telazol--tiletamine and zolazepam by a gas chromatography/mass spectrometry-based method. | 2006-10-02 |
|
| Reversible immobilization of free-ranging African lions (Panthera leo) with medetomidine-tiletamine-zolazepam and atipamezole. | 2006-04 |
|
| Immobilization of free-ranging maned wolf (Chrysocyon brachyurus) with tiletamine and zolazepam in central Brazil. | 2006-03 |
|
| Chemical immobilization of adult female Weddell seals with tiletamine and zolazepam: effects of age, condition and stage of lactation. | 2006-02-09 |
|
| Effects of epidural morphine and transdermal fentanyl analgesia on physiology and behaviour after abdominal surgery in pigs. | 2006-01 |
|
| Clinical and cardiorespiratory effects of propofol in the spotted bamboo shark (Chylloscyllium plagiosum). | 2005-12 |
|
| Reversible anaesthesia of free-ranging lions (Panthera leo) in Zimbabwe. | 2005-12 |
Patents
Sample Use Guides
veterinary:
Dogs: In healthy dogs, an initial intramuscular dosage of 3 to 4.5 mg/lb (6.6 to 9.9 mg/kg) TELAZOL(tiletamine HCl and zolazepam HCl) is recommended for diagnostic purposes; 4.5 to 6 mg/lb (9.9 to 13.2 mg/kg) for minor procedures of short duration, such as treatment of lacerations and wounds, castrations and other procedures requiring mild to moderate analgesia. When supplemental doses of TELAZOL are required, such individual supplemental doses should be less than the initial dose, and the total dose given (initial dose plus supplemental dose or doses) should not exceed 12 mg/lb (26.4 mg/kg). The maximum safe dose is 13.6 mg/lb (29.92 mg/kg).
Cats: In healthy cats, an initial TELAZOL dosage of 4.4 to 5.4 mg/lb (9.7 to 11.9 mg/kg) is recommended for such procedures as dentistry, treatment of abscesses, foreign body removal and related types of surgery; 4.8 to 5.7 mg/lb (10.6 to 12.5 mg/kg) for minor procedures requiring mild to moderate analgesia, such as repair of lacerations, castrations and other procedures of short duration. Initial dosages of 6.5 to 7.2 mg/lb (14.3 to 15.8 mg/kg) are recommended for ovario- hysterectomy and onychectomy. When supplemental doses of TELAZOL are required, such individual supplemental doses should be given in increments that are less than the initial dose, and the total dose given (initial dose plus supplemental doses) should not exceed the maximum allowable safe dose of 32.7 mg/lb (72 mg/kg).
Route of Administration:
Intramuscular
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3320347
Tiletamine was a potent and reversible antagonist of NMA-mediated responses without itself having major effects in low concentrations on normal membrane and synaptic pyramidal cell properties. 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 microM 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 microM, had no effect on the orthodromically elicited excitatory postsynaptic potential, action potential amplitude or duration, resting membrane potential, or input resistance. In Mg++-free perfusate, the excitatory postsynaptic potential was greatly augmented to give a paroxysmal depolarization shift and was reversibly blocked by 10 microM tiletamine.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:58:51 GMT 2025
by
admin
on
Mon Mar 31 17:58:51 GMT 2025
|
| Record UNII |
2YFC543249
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C245
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
7638
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
2YFC543249
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
D013992
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
2820
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
CHEMBL2110703
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
Tiletamine
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
DB11549
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
SUB11050MIG
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
2YFC543249
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
100000082676
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
26533
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
m10862
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | Merck Index | ||
|
C84211
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
1535217
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | RxNorm | ||
|
DTXSID5048552
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
14176-49-9
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY | |||
|
238-031-9
Created by
admin on Mon Mar 31 17:58:51 GMT 2025 , Edited by admin on Mon Mar 31 17:58:51 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
SALT/SOLVATE -> PARENT |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |