N,N'-DISUBSTITUTED ACETAMIDINES AS HIGH-AFFINITY SIGMA-RECEPTOR LIGANDS

Authors
REDDY NL FISCHER JB BURKEHOWIE KJ BARMETTLER P RHODES MR WEBER E KEANA JFW
Citation
Nl. Reddy et al., N,N'-DISUBSTITUTED ACETAMIDINES AS HIGH-AFFINITY SIGMA-RECEPTOR LIGANDS, Bioorganic & medicinal chemistry letters, 3(10), 1993, pp. 2113-2116
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
10
Year of publication
1993
Pages
2113 - 2116
Database
ISI
SICI code
0960-894X(1993)3:10<2113:NAAHSL>2.0.ZU;2-6
Abstract
A series of N,N'-disubstituted acetamidines was prepared as mammalian brain sigma receptor ligands. The in vitro binding affinities of seven representative ligands were measured using guinea pig brain membrane suspensions. N-1-adamantyl-N'-o-tolyl acetamidine is the most potent l igand in the series (IC50 = 6 nM vs [H-3]-DTG). All ligands showed low affinity toward the PCP site.