Kikumoto R, Tobe A, Fukami H, Egawa M
J Med Chem. 1983 Feb;26(2):246-50. doi: 10.1021/jm00356a024.
A series of (omega-piperazinylalkoxy)indan derivatives has been synthesized and screened for potential antianxiety activities. The effect of structural modification of these molecules on activities has been systemically examined. Antianxiety activity was displayed by 5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (2), 5-[3-[4-(4-fluorophenyl)-1-piperazinyl]-propoxy]indan (8), 6-fluoro-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (33), and 6-methyl-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (42), as determined in antifighting and anti-morphine tests. These derivatives in antianxiety tests were equipotent or more potent than chlordiazepoxide with less muscle-relaxant effect. They also showed weak neuroleptic-like action.
已经合成了一系列（ω-哌嗪基烷氧基）茚满衍生物，并对其潜在的抗焦虑活性进行了筛选。系统地研究了这些分子的结构修饰对活性的影响。通过抗争斗和抗吗啡试验确定，5-[3-(4-苯基-1-哌嗪基)丙氧基]茚满（2）、5-[3-[4-(4-氟苯基)-1-哌嗪基]丙氧基]茚满（8）、6-氟-5-[3-(4-苯基-1-哌嗪基)丙氧基]茚满（33）和6-甲基-5-[3-(4-苯基-1-哌嗪基)丙氧基]茚满（42）具有抗焦虑活性。这些衍生物在抗焦虑试验中与氯氮卓效力相当或更强，且肌肉松弛作用较小。它们还表现出微弱的抗精神病样作用。
