Page last updated: 2024-12-06

tiletamine

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Description

Tiletamine: Proposed anesthetic with possible anticonvulsant and sedative properties. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID26533
CHEMBL ID2110703
CHEBI ID94356
SCHEMBL ID115212
MeSH IDM0021530

Synonyms (48)

Synonym
tiletamine
cyclohexanone, 2-(ethylamino)-2-(2-thienyl)-
BSPBIO_001203
NCGC00179264-01
BPBIO1_001325
AB00514642
PRESTWICK3_001022
2-(ethylamino)-2-(2-thienyl)cyclohexanone
tiletamina [inn-spanish]
tiletaminum [inn-latin]
tiletamine [inn:ban]
einecs 238-031-9
SPBIO_003064
PRESTWICK1_001022
PRESTWICK0_001022
PRESTWICK2_001022
D08596
tiletamine (inn)
14176-49-9
AKOS005066229
2-(ethylamino)-2-thiophen-2-ylcyclohexan-1-one
2-(ethylamino)-2-thiophen-2-yl-1-cyclohexanone
2-(ethylamino)-2-thiophen-2-yl-cyclohexan-1-one
A807808
tiletamina
2yfc543249 ,
unii-2yfc543249
tiletaminum
hsdb 7638
BRD-A30582499-003-01-0
tiletamine [who-dd]
tiletamine [hsdb]
tiletamine [mi]
tiletamine [inn]
SCHEMBL115212
DTXSID5048552
CHEMBL2110703
2-(ethylamino)-2-(2-thienyl)cyclohexanone #
QAXBVGVYDCAVLV-UHFFFAOYSA-N
AC-23715
AB00514642_02
J-524970
CHEBI:94356
FT-0756967
14176-49-9 (free base)
DB11549
Q2083144
NCGC00179264-03

Research Excerpts

Overview

Tiletamine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist chemically related to ketamine and phencyclidine. Tiletamine hydrochloride is a lipophilic and potent veterinary anesthetic.

ExcerptReferenceRelevance
"Tiletamine/zolazepam is a dissociative anesthetic combination commonly used in small animals but information is limited in rats. "( Tiletamine/zolazepam and dexmedetomidine with tramadol provide effective general anesthesia in rats.
Durongphongtorn, S; Jampachaisri, K; Limprasutr, V; Pacharinsak, C; Sharp, P, 2021
)
3.51
"Tiletamine-zolazepam is a widely used as an alternative chemical immobilization method in non-human primates, with a safe application pathway and necessary relaxation. "( Electrocardiographic parameters of Sapajus libidinosus (SPIX, 1823) after chemical immobilization with tiletamine-zolazepam.
Andrade, JK; Carreiro, ADN; Costa, TSF; de La Salles, AYF; de Menezes, DJA; de Souza, AP; de Souza, JG; Lemos, KKA; Reinaldo, MPOS, 2019
)
2.17
"Tiletamine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist chemically related to ketamine and phencyclidine. "( Effects of a non-competitive N-methyl-d-aspartate (NMDA) antagonist, tiletamine, in adult zebrafish.
Kalueff, AV; Khatsko, SL; Kolesnikova, TO; Morzherin, YY; Shevyrin, VA,
)
1.81
"Tiletamine is a disassociative anesthetic similar to ketamine and phencyclidine, and zolazepam is a diazepine derivative tranquilizer used to minimize the muscle hypertonicity and seizures associated with tiletamine."( A fatality related to the veterinary anesthetic telazol.
Camporese, T; Cording, CJ; DeLuca, R; Spratt, E, 1999
)
1.02
"Tiletamine hydrochloride is a lipophilic and potent veterinary anesthetic."( Tiletamine is a potent inhibitor of N-methyl-aspartate-induced depolarizations in rat hippocampus and striatum.
Bohacek, R; ffRench-Mullen, JM; Fisher, RS; Lehmann, J, 1987
)
2.44

Treatment

Treatment with tiletamine had a slight, but insignificant, effect on CYP-mediated enzyme activities. Pretreatment did not attenuate the MK-801-induced increases in rat pyriform cortical DA metabolism. This suggests that tiletamines is not a partial agonist of the NMDA-uncoupled PCP recognition sites.

ExcerptReferenceRelevance
"Treatment with tiletamine had a slight, but insignificant, effect on CYP-mediated enzyme activities."( Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol.
Bandiera, SM; Wong, A, 1998
)
0.64
"Pretreatment with tiletamine did not attenuate the MK-801-induced increases in rat pyriform cortical DA metabolism, a result suggesting that tiletamine is not a partial agonist of the NMDA-uncoupled PCP recognition sites in this region."( Contrasting neurochemical interactions of tiletamine, a potent phencyclidine (PCP) receptor ligand, with the N-methyl-D-aspartate-coupled and -uncoupled PCP recognition sites.
Cler, JA; Contreras, PC; Dilworth, VM; Iyengar, S; Mick, SJ; Monahan, JB; Rao, TS; Wood, PL, 1991
)
0.87

Toxicity

ExcerptReferenceRelevance
"The goals of the study were to find a safe intraperitoneal injection anesthesia protocol for medium-duration surgery in mice (e."( Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth.
Arras, M; Autenried, P; Rettich, A; Rülicke, T; Spaeni, D, 2001
)
0.31

Pharmacokinetics

ExcerptReferenceRelevance
"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."( Pharmacokinetics and tissue residues of Telazol in free-ranging polar bears.
Farley, SD; Gorecki, DK; Ramsay, MA; Semple, HA, 2000
)
0.49
" These results collectively point to major pharmacokinetic and metabolic differences between the two components of this fixed-dose anesthetic combination."( Pharmacokinetic study in pigs and in vitro metabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol).
Beilman, GJ; Kaila, N; Kumar, A; Mann, HJ; Remmel, RP, 2014
)
0.6

Compound-Compound Interactions

The goal of this study was to determine whether a drug combination using nalbuphine with dexmedetomidine and tiletamine/zolazepam is non-inferior to one that uses butorphanol.

ExcerptReferenceRelevance
"To evaluate anesthetic effects of tiletamine-zolazepam (TZ), alone or in combination with butorphanol, in goats undergoing laparotomy for embryo collection."( Anesthetic effects of tiletamine-zolazepam, alone or in combination with butorphanol, in goats.
Carroll, GL; Hambleton, R; Hartsfield, SM, 1997
)
0.89
"To evaluate antinociceptive and selected effects associated with IM administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.8
" Procedures-Each llama received tiletamine-zolazepam (2 mg/kg) combined with either xylazine (0."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.88
"Low dose tiletamine-zolazepam combined with methadone provided superior sedation to ACE."( A comparison of low dose tiletamine-zolazepam or acepromazine combined with methadone for pre-anaesthetic medication in cats.
Kloeppel, H; Mair, A; Ticehurst, K, 2014
)
1.12
"The goal of this study was to determine whether a drug combination using nalbuphine with dexmedetomidine and tiletamine/zolazepam is non-inferior to one that uses butorphanol."( Use of nalbuphine as a substitute for butorphanol in combination with dexmedetomidine and tiletamine/zolazepam: a randomized non-inferiority trial.
Cornell, HN; Hofmeister, EH; Kelsey, SE; Kreisler, RE; Smith, VA, 2020
)
0.99
" Each animal was randomly assigned to receive either 80 µg/kg (group L) or 100 µg/kg (group H) medetomidine, combined with 3 mg/kg tiletamine-zolazepam administered intramuscularly."( Comparison of the Cardiovascular Effects of Two Medetomidine Doses Combined with Tiletamine-Zolazepam for the Immobilization of Red Deer Hinds (Cervus elaphus).
Einwaller, J; Habe, M; Painer, J; Pohlin, F; Rauch, H; Stalder, G, 2022
)
1.15

Dosage Studied

A tiletamine/zolazepam combination was used to immobilize 24 captive giant Chacoan peccaries (Catagonus wagneri) at a mean dosage rate of 2. The time of year, most likely associated with differences in ambient temperature and in confinement, influenced the recommended dosage for xylazine and tiletamines.

ExcerptRelevanceReference
"Five anesthetic agents (C1744, etorphine, fentanyl, ketamine hydrochloride, and halothane) were tested to establish the dosage of a safe, effective, short-acting anesthetic for use in the sea otter."( Comparison of anesthetic agents in the sea otter.
Kocher, FH; Williams, TD, 1978
)
0.26
"001) positive linear relationship between duration of anesthesia and dosage for all animals in which the duration was recorded (n = 36)."( Tiletamine and zolazepam for immobilization of wild lions and leopards.
Bertram, BC; Hamilton, PH; King, JM, 1977
)
1.7
" Recordings from CI-744 dosed seals displayed a well-demarcated developmental sequence of VER's, contrary to VER's recorded in flaxedilized seals."( Visual evoked response (VER) changes during maturation in the Weddell seal.
Gruenau, SP; Shurley, JT, 1976
)
0.26
" However, following intracerebroventricular administration (100-500 micrograms/rat), tiletamine increased pyriform cortical DA metabolism with a bell-shaped dose-response curve."( Contrasting neurochemical interactions of tiletamine, a potent phencyclidine (PCP) receptor ligand, with the N-methyl-D-aspartate-coupled and -uncoupled PCP recognition sites.
Cler, JA; Contreras, PC; Dilworth, VM; Iyengar, S; Mick, SJ; Monahan, JB; Rao, TS; Wood, PL, 1991
)
0.77
" The drug was administered intramuscularly in ten dogs at a dosage of 10 mg/kg bwt of tiletamine and 10 mg/kg bwt of zolazepam and tested for its effects on hemodynamics, respiration, and the antagonistic effect of flumazenil."( [Anesthesia in dogs with the combination preparation Tilest 500].
Hess, L, 1991
)
0.5
" Neither dosing regimen caused significant changes in right atrial pressure, heart rate, pulmonary vascular resistance, or pulmonary capillary wedge pressure."( The cardiovascular response of sheep to tiletamine-zolazepam and butorphanol tartrate anesthesia.
Howard, BW; Januszkiewicz, AJ; Lagutchik, MS; Martin, DG,
)
0.4
" Two dosage levels of 12 mg/kg and 22 mg/kg were evaluated."( Evaluation of a combination of tiletamine and zolazepam as an anesthetic for ferrets.
Payton, AJ; Pick, JR, 1989
)
0.56
" Results showed Telazol to be a safe anesthetic and when dosed at 60 mg/kg to be suitable for major surgical procedures."( A new anesthetic agent for use in the gerbil.
Hrapkiewicz, KL; Smiler, KL; Stein, S, 1989
)
0.28
" A dosage of 5 mg/kg of body weight, administered IM, resulted in variable weak tranquilization."( Evaluation of use of tiletamine/zolazepam for anesthesia of bullfrogs and leopard frogs.
Durante, R; Letcher, J, 1995
)
0.61
" Thirteen animals were given an additional dosage of ketamine hydrochloride manually when they recovered from the first injection of TEL."( Field application of Telazol (tiletamine hydrochloride and zolazepam hydrochloride) to immobilize wild red howler monkeys (Alouatta seniculus) in Venezuela.
Agoramoorthy, G; Rudran, R, 1994
)
0.58
" Recovery time varied with weight and dosage of yohimbine."( Immobilization of Rocky Mountain elk with Telazol and xylazine hydrochloride, and antagonism by yohimbine hydrochloride.
Brundige, GC; Hustead, DR; Jenks, JA; Millspaugh, JJ; Tyner, CL, 1995
)
0.29
" The addition of methoxyflurane significantly potentiated the anaesthetic and analgesic properties of the high dosage ketamine-xylazine combination."( Evaluation of anaesthetic regimens in guineapigs.
Crenshaw, D; Hinson, A; Radde, GR; Toth, LA, 1996
)
0.29
" A secondary goal was to compare the effects produced by Telazol and its constituents with those elicited by sodium phenobarbital (PB) using the same dosing regimen."( Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol.
Bandiera, SM; Wong, A, 1998
)
0.3
"Of the 5,766 cats for which dosing records were complete, 4,584 (79."( Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats.
Centonze, LA; Cistola, AM; Levy, JK; Robertson, SA; Williams, LS, 2002
)
0.59
" 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 animals in better body condition."( Response of wild subantarctic fur seal (Arctocephalus tropicalis) females to ketamine and tiletamine-zolazepam anesthesia.
Beauplet, G; Dabin, W; Guinet, C, 2002
)
0.54
" The mean dosage (0."( Tiletamine-zolazepam, ketamine, and xylazine anesthesia of captive cheetah (Acinonyx jubatus).
Bonar, CJ; Evans, SE; Lewandowski, AH, 2002
)
1.76
" Although induction time was similar between drugs, induction dosage and volume were less with XZT."( Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine.
Cattet, MR; Caulkett, NA; Lunn, NJ, 2003
)
0.57
" A combination of 500 mg zolazepam, 500 mg tiletamine, 500 mg xylazine, and 1000 mg (10 ml) ketamine, administered in a dosage of 1 ml per 100-150 kg bodyweight (depending on the species), proved to be most reliable and effective."( [Immobilization of cattle and bison with a combination of xylazine, zolazepam-tiletamine and ketamine].
Hofkes, LM; Hoyer, MJ; Overgaauw, PA; van Dijk, P, 2005
)
0.82
"01) between dosage and time to first effect of immobilants."( Tiletamine-zolazepam-xylazine immobilization of American marten (Martes americana).
Belant, JL, 2005
)
1.77
" There was no relationship between the amount (mg/kg) of Telazol-xylazine injected and time to first effect of immobilants, dosage and time to induction, or between dosage and time to recovery."( Tiletamine-zolazepam-xylazine immobilization of fishers (Martes pennanti).
Belant, JL, 2007
)
1.78
" The total Telazol dosage was also significantly different between young lemurs (33 +/- 15 mg/kg) and mature lemurs (18 +/- 9 mg/kg)."( Field anesthesia of wild ring-tailed lemurs (Lemur catta) using tiletamine-zolazepam, medetomidine, and butorphanol.
Cuozzo, FP; Larsen, RS; Moresco, A; Sauther, ML, 2011
)
0.61
"The objectives of our study were to investigate the dose-response relationship of the TASER X26 discharge duration in an anesthetized swine model."( Repetitive TASER X26 discharge resulted in adverse physiologic events with a dose-response relationship related to the duration of discharge in anesthetized swine model.
Ahn, JH; Choi, SC; Min, YG; Park, EJ, 2013
)
0.39
" In the main trial (romifidine combinations) mean time (minutes) to standing increased with increasing dosage (R40TZ1 13; R80TZ2 32)."( Romifidine and low doses of tiletamine-zolazepam in dogs.
Domínguez, JM; Fernández, A; Gómez-Villamandos, RJ; Granados, MM; López, I; Martínez, C; Morgaz, J; Muñoz, P; Navarrete, R, 2013
)
0.68
" The time of year, most likely associated with differences in ambient temperature and in confinement, influenced the recommended dosage for xylazine and tiletamine-zolazepam in fallow deer."( Influence of Ambient Temperature and Confinement on the Chemical Immobilization of Fallow Deer ( Dama dama ).
Costa, GL; Cucinotta, G; Interlandi, C; Morici, M; Musicò, M; Nastasi, B; Spadola, F, 2017
)
0.65
" The dosage and drug combination used was effective for immobilization of ABBs with minimal adverse effects on vital signs and can be recommended in most clinical applications."( Immobilization of Asiatic Black Bears ( Ursus thibetanus ) with Medetomidine-Zolazepam-Tiletamine in South Korea.
Jeong, DH; Seok, SH; Song, BC; Yang, JJ; Yeon, SC, 2017
)
0.68
"To determine the effective dosage of the combination tiletamine-zolazepam-ketamine-xylazine (TKX), with or without methadone, in dogs."( Determination of the effective dosage of tiletamine-zolazepam-ketamine-xylazine, with or without methadone, in dogs.
Baier, ME; Herrera Becerra, JR; Martins, LGB; Monteiro, ER; Souza, MJ, 2022
)
1.24
" The consistency of respiratory parameters during the entire exposure time is paramount to ensuring dosing accuracy."( Comparison of Alfaxalone-Midazolam, Tiletamine-Zolazepam, and KetamineAcepromazine Anesthesia during Plethysmography in Cynomolgus Macaques (
Astleford, SM; Bowling, PA; Casselman, AM; Dixon, BC; Ghering, JM; Marion, BM; White, CE, 2022
)
1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aralkylamineAn alkylamine in which the alkyl group is substituted by an aromatic group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (340)

TimeframeStudies, This Drug (%)All Drugs %
pre-199035 (10.29)18.7374
1990's96 (28.24)18.2507
2000's89 (26.18)29.6817
2010's88 (25.88)24.3611
2020's32 (9.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.32 (24.57)
Research Supply Index6.04 (2.92)
Research Growth Index4.87 (4.65)
Search Engine Demand Index86.41 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials64 (18.08%)5.53%
Reviews8 (2.26%)6.00%
Case Studies13 (3.67%)4.05%
Observational1 (0.28%)0.25%
Other268 (75.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]