乌美螺酮
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| 临床资料 | |
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| 给药途径 | 口服 |
| ATC码 |
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| 法律规范状态 | |
| 法律规范 |
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| 药物动力学数据 | |
| 生物半衰期 | 未知，但效果比其他阿扎匹隆类药物持续时间更长，在人体临床研究中单剂量后可持续长达23小时。[1] |
| 识别信息 | |
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| CAS号 | 107736-98-1 |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard (EPA) | |
| 化学信息 | |
| 化学式 | C28H40N4O5 |
| 摩尔质量 | 512.65 g·mol−1 |
| 3D模型（JSmol） | |
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乌美螺酮（INN：umespirone；开发代号：KC-9172）是一种阿扎匹隆类药物，具有抗焦虑和抗精神病特性。[2][3][4][5]它是5-HT1A受体部分激动剂（Ki= 5 nM）、D2受体部分激动剂（Ki= 23 nM）和α1-肾上腺素受体拮抗剂（Ki= 14 nM），并且对σ受体也具有弱亲和力（Ki= 558 nM）。[2][6][7]与许多其他抗焦虑药和抗精神病药不同，乌美螺酮产生最小程度的镇静、认知/记忆障碍、僵直和锥体外系症状。[1][5][6]
合成
参见
参考资料
- ^ 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锋ling, H.; Krijzer, F. Drugs Fut 1991,16(5),437.
- ^ DE3529872 idem Uwe Schoen, Wolfgang Kehrbach, Werner Benson, Andreas Fuchs, Michael Ruhland, 美国专利第4,771,044号 (1988 to Kali-Chemie Pharma Gmbh).
