米達西尼
化合物
米達西尼（英語：Imidazenil[1]）是一種實驗性抗焦慮藥，苯二氮䓬類衍生物，與咪達唑侖、氟馬西尼和溴他西尼等其他咪唑並苯二氮䓬類藥物關係最密切。
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| CAS編號 | 151271-08-8  |
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| 化學式 | C18H12BrFN4O |
| 摩爾質量 | 399.22 g·mol−1 |
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米達西尼是一種高效的苯二氮䓬受體部分激動劑，[2]具有不尋常的作用，產生一些與正常苯二氮䓬類藥物相關的作用，例如抗驚厥和抗焦慮作用，但沒有任何顯着的鎮靜或失憶[3]作用。事實上，米達西尼可阻斷地西泮的鎮靜作用，但不會降低驚厥閾值，[4]因此可能是一種比目前常用於治療苯二氮䓬類藥物過量的拮抗劑氟馬西尼更靈活的解毒劑。
米達西尼尚未商業化開發用於人類，但它已被認為是一種安全有效的焦慮治療方法，[5]是一種有效但非鎮靜的抗驚厥藥，可能特別適用於治療有機磷酸鹽神經毒劑中毒，[6][7]並且作為一種治療精神分裂症的新方法。[8]
參見
編輯參考資料
編輯- ^ 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.