Design and synthesis of selective α1B adrenoceptor antagonists

A series of novel indolylpiperidine derivatives were synthesized and assessed for their pharmacological profiles at α1 adrenoceptor subtypes by in vitro binding studies at rat α1A and α1B receptors. Compound 11 was a potent (Ki = 0.63 nM) and selective (approximately 30-fold more selective for the α1B receptor than for the α1A receptor) α1B adrenoceptor antagonist.