Ontology highlight
ABSTRACT:
SUBMITTER: Donohue SR
PROVIDER: S-EPMC2587418 | biostudies-literature | 2008 Sep
REPOSITORIES: biostudies-literature
Donohue Sean R SR Krushinski Joseph H JH Pike Victor W VW Chernet Eyassu E Phebus Lee L Chesterfield Amy K AK Felder Christian C CC Halldin Christer C Schaus John M JM
Journal of medicinal chemistry 20080901 18
We have reported that [methyl- (11)C] (3 R,5 R)-5-(3-methoxyphenyl)-3-[(R)-1-phenylethylamino]-1-(4-trifluoromethylphenyl)pyrrolidin-2-one ([(11)C] 8, [(11)C]MePPEP) binds with high selectivity to cannabinoid type-1 (CB 1) receptors in monkey brain in vivo. We now describe the synthesis of 8 and four analogues, namely, the 4-fluorophenyl (16, FMePPEP), 3-fluoromethoxy (20, FMPEP), 3-fluoromethoxy- d 2 (21, FMPEP- d 2), and 3-fluoroethoxy analogues (22, FEPEP), and report their activity in an ex ...[more]