利卡司琼

利卡司琼
臨床資料
ATC碼
  • 未分配
识别信息
  • endo-N-(8-Methyl-8-azabicyclo[3.2.1]oct-3yl)-2,3-dihydro-3,3-dimethyl-indole-1-carboxamide
CAS号117086-68-7  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
化学信息
化学式C19H27N3O
摩尔质量313.45 g·mol−1
3D模型（JSmol（英语：JSmol））
  • CC1(CN(c2c1cccc2)C(=O)N[C@H]3C[C@H]4CC[C@@H](C3)N4C)C
  • InChI=1S/C19H27N3O/c1-19(2)12-22(17-7-5-4-6-16(17)19)18(23)20-13-10-14-8-9-15(11-13)21(14)3/h4-7,13-15H,8-12H2,1-3H3,(H,20,23)/t13-,14+,15- ☒N
  • Key:ILXWRFDRNAKTDD-QDMKHBRRSA-N ☒N

利卡司琼（INN：ricasetron；开发代号：BRL-46470） 是一种药物，用作血清素5-HT3受体的选择性拮抗剂。[1]它与其他5-HT3拮抗剂一样具有止吐作用，[2]并且具有明显强于其他相关药物的抗焦虑作用，[3]且副作用比苯二氮䓬类抗焦虑药更少。[4][5]然而，它从未被开发用于医疗用途。

参考资料

[编辑]
  1. ^ Newberry NR, Watkins CJ, Sprosen TS, Blackburn TP, Grahame-Smith DG, Leslie RA. BRL 46470 potently antagonizes neural responses activated by 5-HT3 receptors. Neuropharmacology. August 1993, 32 (8): 729–35. PMID 8413836. S2CID 19469831. doi:10.1016/0028-3908(93)90180-B. 
  2. ^ Bermudez J, Sanger GJ. Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets. The Journal of Pharmacy and Pharmacology. June 1994, 46 (6): 520–1. PMID 7932054. S2CID 11799269. doi:10.1111/j.2042-7158.1994.tb03843.x. 
  3. ^ Blackburn TP, Baxter GS, Kennett GA, King FD, Piper DC, Sanger GJ, Thomas DR, Upton N, Wood MD. BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties. Psychopharmacology. 1993, 110 (3): 257–64. PMID 7831418. S2CID 9595942. doi:10.1007/BF02251279. 
  4. ^ Link CG, Leigh TJ, Dennison JK. The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG. British Journal of Clinical Pharmacology. April 1993, 35 (4): 395–9. PMC 1381550 可免费查阅. PMID 8485019. doi:10.1111/j.1365-2125.1993.tb04156.x. 
  5. ^ de Souza Silva M, Guimarães FS, Graeff FG, Tomaz C. Absence of amnestic effect of an anxiolytic 5-HT3 antagonist (BRL 46470A) injected into basolateral amygdala, as opposed to diazepam. Behavioural Brain Research. December 1993, 59 (1–2): 141–5. PMID 8155281. S2CID 3999586. doi:10.1016/0166-4328(93)90160-R.