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Chemical Compound Review

CI-716     6-(2-fluorophenyl)-2,8,10- trimethyl-2,5,9...

Synonyms: Telazol, Zolazepam HCl, SureCN73002, CHEMBL2107559, AR-1L5917, ...
This record was replaced with 35775.
 
 
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Disease relevance of ZOLAZEPAM

  • Adult male rats were given a single intraperitoneal injection of Telazol dose at a of 20, 40, 80, or 120 mg/kg body weight (six rats/dose), while control rats received the vehicle only [1].
  • There are no studies examining spinal toxicity of Telazol, and further studies are necessary before recommending clinical use of this technique [2].
  • We developed a technique using Telazol (13 mg/kg) to anesthetize ducks before surgical biopsy of the liver in ducks infected with duck hepatitis B virus [3].
 

High impact information on ZOLAZEPAM

  • The primary goal of the present study was to determine the constituent of Telazol responsible for the enzyme induction [4].
  • Densitometric quantitation of immunoblots probed with polyclonal antibody against cytochrome P450 2B1 indicated a 17-fold increase in the hepatic level of cytochrome P450 2B1 for rats treated with the highest dose of Telazol [1].
  • Monkeys were anesthetized during experiments with Telazol, a dissociative agent that has no significant effect on microstimulation-induced eye movement parameters (current threshold, velocity, and duration) [5].
  • In the presence of 0.5 mg of anti-cytochrome P450 2B1 IgG/nmol P450, benzyloxyresorufin O-dealkylase activity was inhibited by 92% in hepatic microsomes prepared from a rat treated with Telazol at a dose of 120 mg/kg compared with only 25% inhibition in hepatic microsomes from a control rat [1].
  • In macaques, lymphocyte numbers decreased following afternoon injection of Telazol, ketamine or saline [6].
 

Chemical compound and disease context of ZOLAZEPAM

 

Biological context of ZOLAZEPAM

 

Anatomical context of ZOLAZEPAM

 

Associations of ZOLAZEPAM with other chemical compounds

 

Analytical, diagnostic and therapeutic context of ZOLAZEPAM

  • Densitometric quantitation of immunoblots revealed that the hepatic CYP2B content was elevated by approximately 15-, 22-, and 25-fold, and the hepatic CYP3A content was increased by 2-, 2-, and 8-fold after treatment with zolazepam, Telazol, and PB, respectively [4].
  • Telazol doses of 2.1 to 6.5 mg/kg resulted in a mean (+/- SD) induction time of 2.3 +/- 0.9 min and a mean (+/- SD) immobilization time of 82.2 +/- 28.6 min [17].
  • Our results indicate that Telazol does not produce analgesia in rabbits and is nephrotoxic at both 32 and 64 mg/kg [18].

References

  1. Inductive effect of Telazol on hepatic expression of cytochrome P450 2B in rats. Wong, A., Bandiera, S.M. Biochem. Pharmacol. (1996) [Pubmed]
  2. Epidural administration of tiletamine/zolazepam in horses. Natalini, C.C., Alves, S.D., Guedes, A.G., Polydoro, A.S., Brondani, J.T., Bopp, S. Veterinary anaesthesia and analgesia. (2004) [Pubmed]
  3. A technique for liver biopsy performed in Pekin ducks using anesthesia with Telazol. Carp, N.Z., Saputelli, J., Halbherr, T.C., Mason, W.S., Jilbert, A.R. Lab. Anim. Sci. (1991) [Pubmed]
  4. Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol. Wong, A., Bandiera, S.M. Biochem. Pharmacol. (1998) [Pubmed]
  5. Functionally defined smooth and saccadic eye movement subregions in the frontal eye field of Cebus monkeys. Tian, J.R., Lynch, J.C. J. Neurophysiol. (1996) [Pubmed]
  6. Cortisol responses to immobilization with Telazol or ketamine in baboons (Papio cynocephalus/anubis) and rhesus macaques (Macaca mulatta). Bentson, K.L., Capitanio, J.P., Mendoza, S.P. J. Med. Primatol. (2003) [Pubmed]
  7. Dissociative anaesthesia in free-ranging male koalas and selected marsupials in captivity. Bush, M., Graves, J., O'Brien, S.J., Wildt, D.E. Aust. Vet. J. (1990) [Pubmed]
  8. Thermoregulation in Telazol (CI-744)-anesthetized rhesus monkey (Macaca mulatta). Holmes, K.R., Hunter, W.S. Am. J. Physiol. (1980) [Pubmed]
  9. Telazol and xylazine anesthesia in sheep. Lin, H.C., Tyler, J.W., Wallace, S.S., Thurmon, J.C., Wolfe, D.F. The Cornell veterinarian. (1993) [Pubmed]
  10. Physiological and behavioral responses of gray wolves (Canis lupus) to immobilization with tiletamine and zolazepam. Kreeger, T.J., Seal, U.S., Callahan, M., Beckel, M. J. Wildl. Dis. (1990) [Pubmed]
  11. Pharmacokinetics and tissue residues of Telazol in free-ranging polar bears. Semple, H.A., Gorecki, D.K., Farley, S.D., Ramsay, M.A. J. Wildl. Dis. (2000) [Pubmed]
  12. Immobilization of polar bears (Ursus maritimus) with Telazol in the Canadian Arctic. Stirling, I., Spencer, C., Andriashek, D. J. Wildl. Dis. (1989) [Pubmed]
  13. Effects of telazol and nembutal on retinal responses. Chaudhary, V., Hansen, R., Lindgren, H., Fulton, A. Documenta ophthalmologica. Advances in ophthalmology. (2003) [Pubmed]
  14. Evaluation of a combination of tiletamine and zolazepam as an anesthetic for ferrets. Payton, A.J., Pick, J.R. Lab. Anim. Sci. (1989) [Pubmed]
  15. Immobilization and physiological parameters associated with chemical restraint of wild pigs with Telazol and xylazine hydrochloride. Sweitzer, R.A., Ghneim, G.S., Gardner, I.A., Van Vuren, D., Gonzales, B.J., Boyce, W.M. J. Wildl. Dis. (1997) [Pubmed]
  16. Immobilization of giant Chacoan peccaries (Catagonus wagneri) with a tiletamine hydrochloride/zolazepam hydrochloride combination. Allen, J.L. J. Wildl. Dis. (1992) [Pubmed]
  17. Field immobilization of Ethiopian wolves (Canis simensis). Sillero-Zubiri, C. J. Wildl. Dis. (1996) [Pubmed]
  18. Anesthetic and nephrotoxic effects of Telazol in New Zealand white rabbits. Brammer, D.W., Doerning, B.J., Chrisp, C.E., Rush, H.G. Lab. Anim. Sci. (1991) [Pubmed]
 
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