NOVEL ANTAGONISTS FOR alha1-ADRENOCEPTOR SUBTYPES

α1-Adrenergic receptors (α1-ARs) belong to the seven-transmembranedomainreceptor superfamily and play a primary role in the regulation of severalphysiological processes, particularly in the cardiovascular system. Threedifferent α1-AR subtypes, namely α1A-AR, α1B-AR and α1D-AR, have beencloned and characterised so far. In the past, several non-subtype-selectiveα1-AR antagonists, such as prazosin (the prototype of these substances),doxazosin and terazosin, have been used as effective antihypertensive drugsand, more recently, in the symptomatic treatment of benign prostatic hypertrophy(BPH). Intensive research in academia and pharmaceutical industrieshas led to the discovery of a number of subtype-selective antagonists in thelast decade particularly for the α1A-AR, which seems to be the main subtypeinvolved in bladder outlet obstruction in patients with BPH. This review,which is mainly based on the patent literature (2000 – 2003), is focused onthe recent advances in the development of new subty