Katz R J, Landau P S, Lott M, Bystritsky A, Diamond B, Hoehn-Saric R, Rosenthal M, Weise C
Pharmaceuticals Division, CIBA-GEIGY Corporation, Summit, NJ 07901.
Biol Psychiatry. 1993;34(1-2):41-4. doi: 10.1016/0006-3223(93)90254-b.
Serotonin 1a and serotonin-2 receptors are implicated in anxiety. Serazepine (CGS-15040A, (R,S)-1,3,4,16b-Tetrahydro-2-methyl-2H,10H-indolo[2,1-c] Pyrazino-[1,2-a][1,4] benzodiazepine-16-carboxylic acid, methyl ester hydrochloride]) is a representative of a novel pentacyclic ring system containing a stabilized indole. In chemical assays it was a highly specific inhibitor of serotonin (5-HT2) binding, and it was active in preliminary preclinical assays of anxiolytic potential. This multicenter trial of CGS-15040A in patients with generalized anxiety disorder demonstrated clinical anxiolytic effects consistent with established preclinical effects. Doses greater than or equal to 10 mg reduced Hamilton Anxiety Scale scores. However, the dose-response relationship was nonlinear. Effects appeared primarily related to the psychic components of anxiety.
血清素1a和血清素2受体与焦虑有关。塞拉西平（CGS - 15040A，(R,S)-1,3,4,16b - 四氢 - 2 - 甲基 - 2H,10H - 吲哚并[2,1 - c]吡嗪并[1,2 - a][1,4]苯并二氮杂卓 - 16 - 羧酸甲酯盐酸盐）是一种含有稳定吲哚的新型五环系统的代表药物。在化学分析中，它是血清素（5 - HT2）结合的高度特异性抑制剂，并且在抗焦虑潜力的初步临床前试验中具有活性。这项关于CGS - 15040A治疗广泛性焦虑症患者的多中心试验显示出与既定临床前效果一致的临床抗焦虑作用。剂量大于或等于10毫克可降低汉密尔顿焦虑量表评分。然而，剂量 - 反应关系是非线性的。其作用主要与焦虑的心理成分有关。
