Chemical and Pharmaceutical Bulletin p. 621 - 632 (1999)
Update date:2022-08-05
Topics:
Masaguer, Christian F.
Casariego, Isabel
Ravina, Enrique
We describe the synthesis of 5-aminoethyl- and 6-aminomethyl-4- oxotetrahydroindoles as butyrophenone derivatives in the indole series, as potential atypical antipsychotics. The affinities of these compounds for serotonin (5-HT(2A)) and dopamine (D2) receptors were evaluated in vitro. The ratios of pK(i)'s for 5-HT(2A)/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. Compounds 26e (QF 0408B) and 26f (QF 0409B) showed high affinity for both D2 and 5-HT(2A) receptors, and their Meltzer's ratios were 1.32 and 1.17 respectively, while haloperidol showed a ratio of 0.93.
View MoreGuangzhou Chemical Reagent Factory
Contact:+86-20-8435 9820 or 8435 7345
Address:Southern Guangzhou, Guangdong, China
Contact:+86 512 6287 2180
Address:398 Ruoshui Road, Suzhou Industrial Park, Suzhou, Jiangsu, P. R. China
Contact:+86 021-51698675
Address:1701, Jielong Plaza, No.618 Pingliang Rd, ShangHai,China
Shanghai Synmedia Chemical Co., Ltd
Contact:+86-21-38681880
Address:6th Floor, 11A Building, No.528 Ruiqing Road, Heqing town, Pudong new district, Shanghai China
website:http://www.amadischem.com
Contact:86-571-89925085
Address:Watts Cosine.No.166.Xiangmao Road.
Doi:10.1039/C2969000598b
(1969)Doi:10.1016/S0040-4020(01)82885-4
(1969)Doi:10.1002/jps.2600571038
(1968)Doi:10.1080/00021369.1977.10862474
(1977)Doi:10.1016/S0040-4039(01)88120-X
(1969)Doi:10.3390/molecules181011783
(2013)
