Journal of Medicinal Chemistry p. 4683 - 4689 (1992)
Update date:2022-08-29
Topics:
Kimes, Alane S.
Wilson, Alan A.
Scheffel, Ursula
Campbell, Bruce G.
London, Edythe D.
An analog of 1,3-di-o-tolylguanidine (DTG), <125I>-labeled 1-(p-iodophenyl)-3-(1-adamantyl)guanidine (PIPAG), was synthesized as a potential ligand for cerebral ? binding sites.Data from in vitro binding experiments and in vivo experiments on brain distribution suggested that PIPAG binds to ? binding sites with high affinity (Kd in low nanomolar range) as determined by Scatchard analysis and relative potencies of ?-specific drugs.Haloperidol had the highest potency to inhibit <125I>PIPAG binding.It was followed by DTG, BMY 14802, and (+)-N-allylnormetazocine.Compounds with high affinities for dopamine receptors (but low affinity for ? binding sites), for opioid receptors, for nicotinic acetylcholine receptors, and for phencyclidine receptors were ineffective inhibitors of <125I>PIPAG binding.
View MoreShanghai Sinofluoro Scientific Co., Ltd
Contact:+86-21-64279360
Address:Room 1006,Building 3,#58 East Xinjian Road, Shanghai ,201100,China,
Contact:+86-21-61318535
Address:Building 29,No.2139 Xizha Road, Fengxian District, Shanghai
Contact:+86 021-51698675
Address:1701, Jielong Plaza, No.618 Pingliang Rd, ShangHai,China
Lonzeal Pharmaceuticals Co., Ltd.
website:http://www.lonzeal.com
Contact:+86-13381011962
Address:RM 801, Yue MOMA, No. 26 Anningzhuang Rd. Haidian District, Beijing, China
Shandong Loyal Chemical industrial Co.,Ltd
Contact:0533-7451788
Address:Linzi Chemical Industrial Park, Zibo, Shandong Province
Doi:10.1002/pola.27972
(2016)Doi:10.1021/acs.jmedchem.7b00950
(2017)Doi:10.1002/jccs.199700062
(1997)Doi:10.1246/cl.1985.669
(1985)Doi:10.1039/f19807600746
(1980)Doi:10.1021/ja00532a046
(1980)