烏美螺酮
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| 臨床資料 | |
|---|---|
| 給藥途徑 | 口服 |
| ATC碼 |
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| 法律規範狀態 | |
| 法律規範 |
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| 藥物動力學數據 | |
| 生物半衰期 | 未知，但效果比其他阿扎匹隆類藥物持續時間更長，在人體臨床研究中單劑量後可持續長達23小時。[1] |
| 識別資訊 | |
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| CAS號 | 107736-98-1 |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard (EPA) | |
| 化學資訊 | |
| 化學式 | C28H40N4O5 |
| 摩爾質量 | 512.65 g·mol−1 |
| 3D模型（JSmol） | |
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烏美螺酮（INN：umespirone；開發代號：KC-9172）是一種阿扎匹隆類藥物，具有抗焦慮和抗精神病特性。[2][3][4][5]它是5-HT1A受體部分激動劑（Ki= 5 nM）、D2受體部分激動劑（Ki= 23 nM）和α1-腎上腺素受體拮抗劑（Ki= 14 nM），並且對σ受體也具有弱親和力（Ki= 558 nM）。[2][6][7]與許多其他抗焦慮藥和抗精神病藥不同，烏美螺酮產生最小程度的鎮靜、認知/記憶障礙、僵直和錐體外系症狀。[1][5][6]
合成
[編輯]
參見
[編輯]參考資料
[編輯]- ^ 1.0 1.1 Holland RL, Wesnes K, Dietrich B. Single dose human pharmacology of umespirone. European Journal of Clinical Pharmacology. 1994, 46 (5): 461–8. PMID 7957544. S2CID 12117650. doi:10.1007/bf00191912.
- ^ 2.0 2.1 Barnes NM, Costall B, Domeney AM, et al. The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacology Biochemistry and Behavior. September 1991, 40 (1): 89–96. PMID 1685786. S2CID 9762359. doi:10.1016/0091-3057(91)90326-W.
- ^ Ruhland M, Krähling H, Fuchs A, Schön U. KC 9172 (free base of KC 7218)--an antipsychotic/anxiolytic compound. I. Antipsychotic and anxiolytic activity in comparison with chlorpromazine, clozapine, diazepam and buspirone. Pharmacopsychiatry. November 1988, 21 (6): 396–8. PMID 2907649. S2CID 260241523. doi:10.1055/s-2007-1017024.
- ^ Krähling H, Fuchs A, Ruhland M, Schön U, Mol F, Tulp M. KC 9172 (free base of KC 7218)--an antipsychotic/anxiolytic compound. II. Discrimination from typical neuroleptics and benzodiazepine-like minor tranquilizers. Pharmacopsychiatry. November 1988, 21 (6): 399–401. PMID 2907650. S2CID 260241655. doi:10.1055/s-2007-1017025.
- ^ 5.0 5.1 Schmidt WJ, Krähling H, Ruhland M. Antagonism of AP-5-induced sniffing stereotypy links umespirone to atypical antipsychotics. Life Sciences. 1991, 48 (6): 499–505. PMID 1671523. doi:10.1016/0024-3205(91)90464-M.
- ^ 6.0 6.1 Ahlenius S, Wijkström A. Mixed agonist-antagonist properties of umespirone at neostriatal dopamine receptors in relation to its behavioral effects in the rat. European Journal of Pharmacology. November 1992, 222 (1): 69–74. PMID 1361441. doi:10.1016/0014-2999(92)90464-F.
- ^ Itzhak Y, Ruhland M, Krähling H. Binding of umespirone to the sigma receptor: evidence for multiple affinity states. Neuropharmacology. February 1990, 29 (2): 181–4. PMID 1970425. S2CID 54326248. doi:10.1016/0028-3908(90)90058-Y
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- ^ Kr鋒ling, H.; Krijzer, F. Drugs Fut 1991,16(5),437.
- ^ DE3529872 idem Uwe Schoen, Wolfgang Kehrbach, Werner Benson, Andreas Fuchs, Michael Ruhland, 美國專利第4,771,044號 (1988 to Kali-Chemie Pharma Gmbh).
