卡他唑酯
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| 临床资料 | |
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| 给药途径 | 口服 |
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| 法律规范状态 | |
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| 识别信息 | |
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| CAS号 | 34966-41-1 |
| PubChem CID | |
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| CompTox Dashboard (EPA) | |
| 化学信息 | |
| 化学式 | C15H22N4O2 |
| 摩尔质量 | 290.37 g·mol−1 |
| 3D模型（JSmol） | |
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卡他唑酯（英语：Cartazolate，开发代号：SQ-65,396）是一种吡唑并吡啶类药物。它作为复合物巴比妥结合位点的 GABAA受体正向变构调节剂，对动物具有抗焦虑作用。[1][2][3][4]它还可作为A1和A2亚型的腺苷拮抗剂以及磷酸二酯酶抑制剂。[5][6]卡他唑酯经过人体临床试验，发现对焦虑症有效，但从未上市。[7]它是由E.R. Squibb and Sons的团队于1970年代开发的。[8]
参见
[编辑]参考资料
[编辑]- ^ Placheta P, Karobath M. In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes. European Journal of Pharmacology. March 1980, 62 (2–3): 225–8. PMID 6103810. doi:10.1016/0014-2999(80)90281-2.
- ^ Supavilai P, Karobath M. Action of pyrazolopyridines as modulators of [3H]flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum. European Journal of Pharmacology. March 1981, 70 (2): 183–93. PMID 6114867. doi:10.1016/0014-2999(81)90213-2.
- ^ Leeb-Lundberg F, Snowman A, Olsen RW. Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites. Journal of Neuroscience. May 1981, 1 (5): 471–7. PMC 6564167
. PMID 7050308. doi:10.1523/JNEUROSCI.01-05-00471.1981 .
- ^ Bristow DR, Martin IL. Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor. Journal of Neurochemistry. March 1990, 54 (3): 751–61. PMID 2154549. S2CID 25784613. doi:10.1111/j.1471-4159.1990.tb02315.x.
- ^ Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D. Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors. Biochemical Pharmacology. February 1988, 37 (4): 655–64. PMC 3445624 . PMID 2829919. doi:10.1016/0006-2952(88)90139-6.
- ^ Wachtel H. Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors. Psychopharmacology. 1982, 77 (4): 309–16. PMID 6182575. S2CID 10122417. doi:10.1007/BF00432761.
- ^ O'Brien, Robert. Receptor binding in drug research. New York: Dekker. 1986: 519. ISBN 0-8247-7548-1.
- ^ US 3966746,Hoehn, Hans & Theodor Denzel,“Amino derivatives of pyrazolopyridine carboxamides”,发表于1976-06-29
