1. The contractile activity, binding activity and localization of endo
thelin (ET)-1 were evaluated in human nonhyperplastic (control) and hy
perplastic prostates. 2. ET-1 caused contraction of both prostates in
a dose-dependent manner. However, this contraction was markedly decrea
sed in hyperplastic prostates. 3. B-max and K-d values of hyperplastic
prostates were greater than those of the control. 4. The muscle and p
roliferative epithelium of hyperplastic prostates showed strong staini
ng for the anti-ET-1 antibody. However, the glandular epithelium of co
ntrol prostates was weakly stained. 5. These findings indicate that re
sponsiveness to ET-1 is decreased, though the ET-1 and ET-1 receptors
increase in the hyperplastic prostate. Namely, the increase in ET-1 re
ceptors is not effective in regulating the contractile response of the
prostate, because its expression is rather dominant in proliferated g
land. 6. These suggest-that ET-1 may not have an important role in the
release of the obstructive symptoms of benign prostatic hypertrophy.