Identification of a Dihydropyridine as a Potent α1a Adrenoceptor-Selective Antagonist That Inhibits Phenylephrine-Induced Contraction of the Human Prostate

Publisher Website
Google Scholar
Abstract
A number of novel dihydropyridine derivatives based upon 1,4-dihydro-3-(methoxycarbonyl)-2,6-dimethyl-4-(4-nitrophenyl)-5-((3-(4,4-diphenylpiperidin-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 (1 9) displayed good binding affinity and selectivity for the α1a adrenoceptor (pKi = 8.73) and potently inhibited (pA2 = 9.23) phenylephrine-induced contraction of the human prostate.