Identification of a dihydropyridine as a potent α(1a) adrenoceptor- selective antagonist that inhibits phenylephrine-induced contraction of the human prostate

Article abstract of DOI:10.1021/jm980077m

A number of novel dihydropyridine derivatives based upon 1,4-dihydro-3- (methoxycarbonyl)-2,6-dimethyl-4-(4-nitrophenyl)-5-((3-(4,4- dihyphenylpiperidin-1-yl)propyl)aminocarbonyl)pyridine (4) have been synthesized and tested at cloned human α adrenoceptors as well as the rat L- type calcium channel. Within this compound series, 5-(aminocarbonyl)-1,4- dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3-((3-(4,4-diphenylpiperidin-1- yl)propyl)aminocarbonyl)pyridine (19)displayed good binding affinity and selectivity for the α(1a) adrenoceptor (pK(i) = 8.73) and potently inhibited (pA₂ = 9.23) phenylephrine-induced contraction of the human prostate.