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Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.

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 alpha 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 alpha1a adrenoceptor (pKi = 8.73) and potently inhibited (pA2 = 9.23) phenylephrine-induced contraction of the human prostate.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Wong WC,Chiu G,Wetzel JM,Marzabadi MR,Nagarathnam D,Wang D,Fang J,Miao SW,Hong X,Forray C,Vaysse PJ,Branchek TA,Gluchowski C,Tang R,Lepor H

doi

10.1021/jm980077m

subject

Has Abstract

pub_date

1998-07-02 00:00:00

pages

2643-50

issue

14

eissn

0022-2623

issn

1520-4804

pii

jm980077m

journal_volume

41

pub_type

杂志文章

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