唑拉西泮

唑拉西泮
临床资料
商品名（英语：Drug nomenclature）	Telazol（与替来他明联合使用）
AHFS/Drugs.com	国际药品名称
ATC码	未分配;
法律规范状态
法律规范	澳：限医生处方（S4）; 美：附表III（与替来他明合用）;
识别信息
	IUPAC命名法 4-(2-fluorophenyl)-1,3,8-trimethyl-6H-pyrazolo[3,4-e][1,4]diazepin-7-one; ;
CAS号	31352-82-6
PubChem CID	35775;
ChemSpider	32907 ;
UNII	G1R474U58U;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID30185278 ;
ECHA InfoCard	100.118.306
化学信息
化学式	C15H15FN4O
摩尔质量	286.31 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES FC1=CC=CC=C1C2=NCC(N(C)C3=C2C(C)=NN3C)=O;
	InChI InChI=1S/C15H15FN4O/c1-9-13-14(10-6-4-5-7-11(10)16)17-8-12(21)19(2)15(13)20(3)18-9/h4-7H,8H2,1-3H3 ; Key:GDSCFOSHSOWNDL-UHFFFAOYSA-N ;

唑拉西泮（英语：Zolazepam^[2]）是一种吡唑并二氮杂䓬酮衍生物，在结构上与苯二氮䓬类药物相关，在兽医学中用作多种动物的麻醉剂。唑拉西泮通常与其他药物联合使用，例如NMDA 拮抗剂替来他明或α2肾上腺素能受体激动剂甲苯噻嗪，具体取决于其用途。它的效力大约是地西泮的四倍（在动物模型中为0.32mg/kg对比1.2mg/kg），但它在生理pH值下既是水溶性的又是非离子化的，这意味着它的起效非常快。^[3]

唑拉西泮由霍勒斯·德瓦尔德和唐纳德·巴特勒为帕克-戴维斯开发，^[4]是对苯二氮䓬结构进行非常详细分析的结果（1969年美国专利第3,558,605号）。

唑拉西泮与替来他明的联合使用，已被用于镇静野生动物，例如大猩猩和北极熊，并且由于副作用减少而被发现优于氯胺酮。^[5]^[6]唑拉西泮和替来他明的1:1混合物以商品名Telazol和Zoletil出售。

参见

苯二氮䓬类

参考资料

^ Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III (PDF). Isomer Design. Drug Enforcement Administration. January 21, 1987 [January 16, 2023]. （原始内容存档 (PDF)于March 3, 2022）.
^ US 3879535,Stoliker, Harry E.,“Anesthetic compositions and methods of use”,发表于1975-04-22
^ DeWald HA, Lobbestael S, Butler DE. 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. December 1977, 20 (12): 1562–9. PMID 22748. doi:10.1021/jm00222a005.
^ DE 2023453,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]”,发表于1970-11-19
^ Sleeman JM, Cameron K, Mudakikwa AB, Nizeyi JB, Anderson S, Cooper JE, et al. Field anesthesia of free-living mountain gorillas (Gorilla gorilla beringei) from the Virunga Volcano region, Central Africa. Journal of Zoo and Wildlife Medicine. March 2000, 31 (1): 9–14. PMID 10884117. S2CID 20623485. doi:10.1638/1042-7260(2000)031[0009:faoflm]2.0.co;2.
^ Cattet MR, Caulkett NA, Polischuk SC, Ramsay MA. Anesthesia of polar bears (Ursus maritimus) with zolazepam-tiletamine, medetomidine-ketamine, and medetomidine-zolazepam-tiletamine. Journal of Zoo and Wildlife Medicine. September 1999, 30 (3): 354–60. PMID 10572857.

[1] Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III (PDF). Isomer Design. Drug Enforcement Administration. January 21, 1987 [January 16, 2023]. （原始内容存档 (PDF)于March 3, 2022）.

[2] US 3879535,Stoliker, Harry E.,“Anesthetic compositions and methods of use”,发表于1975-04-22

[Horace-3] DeWald HA, Lobbestael S, Butler DE. 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. December 1977, 20 (12): 1562–9. PMID 22748. doi:10.1021/jm00222a005.

[4] DE 2023453,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]”,发表于1970-11-19

[5] Sleeman JM, Cameron K, Mudakikwa AB, Nizeyi JB, Anderson S, Cooper JE, et al. Field anesthesia of free-living mountain gorillas (Gorilla gorilla beringei) from the Virunga Volcano region, Central Africa. Journal of Zoo and Wildlife Medicine. March 2000, 31 (1): 9–14. PMID 10884117. S2CID 20623485. doi:10.1638/1042-7260(2000)031[0009:faoflm]2.0.co;2.

[6] Cattet MR, Caulkett NA, Polischuk SC, Ramsay MA. Anesthesia of polar bears (Ursus maritimus) with zolazepam-tiletamine, medetomidine-ketamine, and medetomidine-zolazepam-tiletamine. Journal of Zoo and Wildlife Medicine. September 1999, 30 (3): 354–60. PMID 10572857.

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