MUSCARINIC RECEPTOR SUBTYPES IN THE RAT PROSTATE-GLAND

Citation
Wak. Lau et Jn. Pennefather, MUSCARINIC RECEPTOR SUBTYPES IN THE RAT PROSTATE-GLAND, European journal of pharmacology, 343(2-3), 1998, pp. 151-156
Citations number
24
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00142999
Volume
343
Issue
2-3
Year of publication
1998
Pages
151 - 156
Database
ISI
SICI code
0014-2999(1998)343:2-3<151:MRSITR>2.0.ZU;2-N
Abstract
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.