BACKGROUND. alpha(1)-adrenoceptor antagonists (blockers) are now commo
nly used in the treatment of the symptoms of lower urinary tract obstr
uction. Originally phenoxybenzamine, a non-selective antagonist at bot
h alpha(1)- and alpha(2)-adrenoceptors, was used by Marco Caine. In an
attempt to minimize side effects, selective alpha(1)-antagonists, e.g
, prazosin, were subsequently developed. More recently, agents such as
alfuzosin, doxazosin, terazosin, and tamsulosin have been introduced
and claims of ''uroselectivity'' and ''prostate'' selectivity have eme
rged. METHODS. This review attempts to put these claims into perspecti
ve and represents a comprehensive analysis of all pre-clinical and cli
nical data including several papers from the Japanese literature. An a
ttempt is made to define what is meant by selectivity at various level
s including the test tube, in the laboratory animal and, most importan
tly, in the clinical context of the whole patient. CONCLUSIONS. The co
nclusions are interpreted within the context of the subdivision of the
alpha(1)-adrenoceptor into alpha(1A), alpha(1B), and alpha(1D) subtyp
es. (C) 1997 Wiley-Liss, Inc.