European Journal of Medicinal Chemistry p. 385 - 396 (1997)
Update date:2022-09-26
Topics:
De Paulis
Hewlett
Schmidt
Mason
Trivedi
Ebert
(S)-5-Iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine. [125I]Iodode-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a K(D) of 1.37 ± 0.21 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor affinities were determined by inhibition of [125I]-MIZAC binding. Optimal affinity for the receptor was obtained with small, electron-withdrawing substituents in the aromatic 5-position and with bulky substituents in the 3-position. [125I]-MIZAC is a selective radioligand useful for in vitro identification of the 5-HT-3 receptor.
View MoreHunan Zhongqi Pharmaceutical Co., Ltd
website:http://www.hnzqzy.com
Contact:0730-8722288 13807308622
Address:Wanjiafan Road ,Yueyang Economic And Technological Development Zone ,Hunan,PRC
Contact:+1-416-493-6870
Address:Toronto, Canada
Jiangxi Huashi Pharmaceutical Co., Ltd
Contact:+86-795-4509628
Address:Ningbo Ave., Fengtian Industrial Park, Fengxin Country, Jiangxi, China.
Contact:+0086-21-61984905-1
Address:Building 60,Zimian Park, LongYang industrial Area, 1515Nong,Yuandong Road Fengxian District, Shanghai ,China
ShangHai Original Economy-Trade Develop Co.,Ltd.,
Contact:86-21-68552131
Address:shanghai
Doi:10.1021/jo00836a006
(1970)Doi:10.1021/jm990617v
(2000)Doi:10.1021/acs.orglett.9b01765
(2019)Doi:10.1016/S0040-4039(00)71120-8
(1980)Doi:10.1016/S0040-4020(00)00011-9
(2000)Doi:10.1016/S0020-1693(99)00531-9
(2000)