乌美螺酮

乌美螺酮
臨床資料
给药途径口服
ATC碼
  • 未分配
法律規範狀態
法律規範
  • 不受管制
藥物動力學數據
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
  • 3-butyl-7-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]-9,9-dimethyl-3,7-diazabicyclo[3.3.1]nonane-2,4,6,8-tetrone
CAS号107736-98-1
PubChem CID
ChemSpider
UNII
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C28H40N4O5
摩尔质量512.65 g·mol−1
3D模型（JSmol（英语：JSmol））
  • O=C1N(C(=O)C2C(=O)N(C(=O)C1C2(C)C)CCCCN4CCN(c3ccccc3OC)CC4)CCCC

乌美螺酮（INN：umespirone；开发代号：KC-9172）是一种阿扎匹隆（英语：Azapirone）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（英语：Catalepsy）和锥体外系症状。[1][5][6]

合成

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合成：[8]专利：[9]

参见

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参考资料

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  1. ^ 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. ^ 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. 
  3. ^ 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. 
  4. ^ 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. ^ 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. ^ 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. 
  7. ^ 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 可免费查阅. 
  8. ^ Kr鋒ling, H.; Krijzer, F. Drugs Fut 1991,16(5),437.
  9. ^ DE3529872 idem Uwe Schoen, Wolfgang Kehrbach, Werner Benson, Andreas Fuchs, Michael Ruhland, 美國專利第4,771,044号 (1988 to Kali-Chemie Pharma Gmbh).