Muscarinic receptor subtypes mediating carbachol-induced contractions
of the rat prostatic smooth muscle were determined. The rank order of
potency of muscarinic receptor antagonists in blocking the effects of
carbachol was (mean pK(B) estimates in parentheses): atropine (8.90) m
uch greater than para-fluorohexahydrosiladifenidol (7.75) greater than
or equal to hexahydrosiladifenidol (7.62) > methoctramine (6.89) grea
ter than or equal to pirenzepine (6.68) greater than or equal to himba
cine (6.67). The specific binding of [H-3]quinuclidinyl benzilate to t
he rat prostatic homogenates was competitively inhibited by (mean pK(i
) values in parentheses): atropine (8.89) much greater than hexahydros
iladifenidol (7.86) > para-fluorohexahydrosiladifenidol (7.28) greater
than or equal to himbacine (7.22) > pirenzepine (6.63) greater than o
r equal to methoctramine (6.38). These profiles, whilst different, ind
icate the probable involvement of muscarinic M-3 receptors in the carb
achol-induced contraction. (C) 1998 Elsevier Science B.V.