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 ...