Chemical and Pharmaceutical Bulletin p. 534 - 541 (1996)
Update date:2022-09-26
Topics:
Ravina, Enrique
Fueyo, Javier
Masaguer, Christian F.
Negreira, Jesus
Cid, Jose
Loza, Isabel
Honrubia, Angeles
Tristan, Helena
Ferreiro, Tomas G.
Fontenla, Jose A.
Rosa, Elizabeth
Calleja, Jose M.
De Ceballos, Maria L.
Starting from benzo- or thienocycloalkaneacetic acids, we have prepared a series of 1-(3-p-fluorobenzoylpropyl)-4-(1-oxo-benzo- or thienocycloalkyl-2-ethyl)piperazines 8a - e containing both semirigid and linear butyrophenones pharmacophores. The affinities of these compounds for dopamine (D2) and 5-hydroxytryptamine (5-HT2A) receptors were evaluated in vitro in receptor-binding assays and in functional experiments. The ratios of pKi's for 5-HT2A/D2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values >1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. The new molecules had a ratio in the range of 0.96-1.11 while haloperidol showed a ratio of 0.93. The 2-piperazinoethyl thiotetralone derivative 8d (QF 0506B) with a ratio of 1.11 was the most active compound.
View MoreContact:021-36356756
Address:Room601,Building No.14,280 Yangcheng Road,Shanghai
Liao Cheng All Win Chemicals Co.,LTD
Contact:86+0635-2991582
Address:Room 402,Unit 1,No.27 building.Zhong tong shi dai haoyuan,liaocheng city,Shan dong Province.China
Contact:+86-10-59484199
Address:No.58-A1026 Liangguan Street
Nanjing Spring & Autumn Biological Engineering Co., Ltd.
Contact:86-180510-83338
Address:Suite# 210, No. 1 BuildingNanjing Agricultural Biotechnology High-tech Entrepreneurship Center, No. 4 Tongwei Road, Xuanwu District, Nanjing,China
Contact:+86-511-88790000
Address:338 North Yushan Rd, Zhenjiang, Jiangsu 212016
Doi:10.1016/S0040-4020(01)96404-X
(1985)Doi:10.1021/ja3083818
(2012)Doi:10.1016/S0008-6215(00)90756-0
(1985)Doi:10.1016/S0040-4020(01)98496-0
(1964)Doi:10.1016/j.poly.2007.09.020
(2008)Doi:10.1021/jo00009a010
(1991)
