Synthesis, pharmacology and pharmacokinetics of 3-(4-Aryl-piperazin-1-ylalkyl)-uracils as uroselective α 1A-antagonists

…, A Guzman, S Jaime-Figueroa, JR Jasper…

Index: Lopez; Arias; Chan; Clarke; Elworthy; Ford; Guzman; Jaime-Figueroa; Jasper; Morgans Jr.; Padilla; Perez-Medrano; Quintero; Romero; Sandoval; Smith; Williams; Blue Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 11 p. 1873 - 1878

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Citation Number: 18

Abstract

Predominance in the urethra and prostate of the α1A-adrenoceptor subtype, which is believed to be the receptor mediating noradrenaline induced smooth muscle contraction in these tissues, led to the preparation of α1A-selective antagonists to be tested as uroselective compounds for the treatment of benign prostatic hyperplasia. Thus, a number of selective α1A-adrenoceptor antagonists were synthesized and assayed in vitro for potency and ...

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