Chemistry:Zolazepam
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| Trade names | Telazol (in combination with tiletamine) |
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| Formula | C15H15FN4O |
| Molar mass | 286.310 g·mol−1 |
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Zolazepam[2] (Flupyrazapon) is a pyrazolodiazepinone derivative structurally related to the benzodiazepine drugs, which is used as an anaesthetic for a wide range of animals in veterinary medicine. Zolazepam is usually administered in combination with other drugs such as the NMDA antagonist tiletamine or the α2 adrenergic receptor agonist xylazine, depending on what purpose it is being used for. It is around four times the potency of diazepam (0.32 mg/kg versus 1.2 mg/kg in animal models) but it is both water-soluble and un-ionized at physiological pH meaning that its onset is very fast.[3]
Zolazepam was developed by Horace A. de Wald and Donald E. Butler for Parke-Davis[4] and was the result of a very detailed analysis of the benzodiazepine structure (U.S. Patent 3,558,605 filed in 1969).
Zolazepam, in combination with tiletamine, has been used in the tranquilization of wild animals, such as gorillas and polar bears, and has been found to be superior to ketamine because of reduced side-effects.[5][6] A 1:1 mixture of zolazepam and tiletamine is sold under the names Telazol and Zoletil.
See also
References
- ↑ "Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III". Drug Enforcement Administration. January 21, 1987. http://isomerdesign.com/Cdsa/FR/52FR2221.pdf.
- ↑ Stoliker, Harry E., "Anesthetic compositions and methods of use", US patent 3879535, published 1975-04-22
- ↑ "Pyrazolodiazepines. 2. 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agents". Journal of Medicinal Chemistry 20 (12): 1562–9. December 1977. doi:10.1021/jm00222a005. PMID 22748.
- ↑ DeWald, Horace Albert & Donald Eugene Butler, "Pyrazolo[3,4-e],[1,4]diazepin-7(1H)-on Verbindungen und ihre pharmazeutisch zulässigen Salze [Pyrazolo[3,4-e],[1.4]diazepin-7(lH)-one compounds and their pharmaceutically acceptable salts]", DE patent 2023453, published 1970-11-19
- ↑ "Field anesthesia of free-living mountain gorillas (Gorilla gorilla beringei) from the Virunga Volcano region, Central Africa". Journal of Zoo and Wildlife Medicine 31 (1): 9–14. March 2000. doi:10.1638/1042-7260(2000)031[0009:faoflm2.0.co;2]. PMID 10884117.
- ↑ "Anesthesia of polar bears (Ursus maritimus) with zolazepam-tiletamine, medetomidine-ketamine, and medetomidine-zolazepam-tiletamine". Journal of Zoo and Wildlife Medicine 30 (3): 354–60. September 1999. PMID 10572857.
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