米达西尼
化合物
米达西尼（英语：Imidazenil[1]）是一种实验性抗焦虑药，苯二氮䓬类衍生物，与咪达唑仑、氟马西尼和溴他西尼等其他咪唑并苯二氮䓬类药物关系最密切。
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| CAS号 | 151271-08-8  |
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| 化学式 | C18H12BrFN4O |
| 摩尔质量 | 399.22 g·mol−1 |
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米达西尼是一种高效的苯二氮䓬受体部分激动剂，[2]具有不寻常的作用，产生一些与正常苯二氮䓬类药物相关的作用，例如抗惊厥和抗焦虑作用，但没有任何显着的镇静或失忆[3]作用。事实上，米达西尼可阻断地西泮的镇静作用，但不会降低惊厥阈值，[4]因此可能是一种比目前常用于治疗苯二氮䓬类药物过量的拮抗剂氟马西尼更灵活的解毒剂。
米达西尼尚未商业化开发用于人类，但它已被认为是一种安全有效的焦虑治疗方法，[5]是一种有效但非镇静的抗惊厥药，可能特别适用于治疗有机磷酸盐神经毒剂中毒，[6][7]并且作为一种治疗精神分裂症的新方法。[8]
参见
编辑参考资料
编辑- ^ US 5317018
- ^ Thompson DM, Auta J, Guidotti A, Costa E. Imidazenil, a new anxiolytic and anticonvulsant drug, attenuates a benzodiazepine-induced cognition deficit in monkeys. The Journal of Pharmacology and Experimental Therapeutics. June 1995, 273 (3): 1307–12. PMID 7791102.
- ^ Auta J, Faust WB, Lambert P, Guidotti A, Costa E, Moerschbaecher JM. Comparison of the effects of full and partial allosteric modulators of GABA(A) receptors on complex behavioral processes in monkeys. Behavioural Pharmacology. June 1995, 6 (4): 323–332. PMID 11224341. S2CID 24584434. doi:10.1097/00008877-199506000-00003.
- ^ Auta J, Costa E, Davis JM, Guidotti A. Imidazenil: an antagonist of the sedative but not the anticonvulsant action of diazepam. Neuropharmacology. September 2005, 49 (3): 425–9. PMID 15964602. S2CID 44619421. doi:10.1016/j.neuropharm.2005.04.005.
- ^ Atack JR. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Current Drug Targets. CNS and Neurological Disorders. August 2003, 2 (4): 213–32. PMID 12871032. doi:10.2174/1568007033482841.
- ^ Rump S, Gidynska T, Galecka E, Antkowiak O, Nawrocka M, Kowalczyk M. Effects of imidazenil, a new benzodiazepine receptor partial agonist, in the treatment of convulsions in organophosphate intoxications. Neurotoxicity Research. 2000, 2 (1): 17–22. PMID 15545002. S2CID 2066413. doi:10.1007/bf03033323.
- ^ Auta J, Costa E, Davis J, Guidotti A. Imidazenil: a potent and safe protective agent against diisopropyl fluorophosphate toxicity. Neuropharmacology. March 2004, 46 (3): 397–403. PMID 14975695. S2CID 41221807. doi:10.1016/j.neuropharm.2003.09.010.
- ^ Guidotti A, Auta J, Davis JM, Dong E, Grayson DR, Veldic M, et al. GABAergic dysfunction in schizophrenia: new treatment strategies on the horizon. Psychopharmacology. July 2005, 180 (2): 191–205. PMID 15864560. S2CID 25147595. doi:10.1007/s00213-005-2212-8.