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PMID: 12540518 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

The Rho-kinase inhibitor Y-27632 and the soluble guanylyl cyclase activator BAY41-2272 relax rabbit vaginal wall and clitoral corpus cavernosum.

British journal of pharmacology ·Vol. 138 ·No. 2 ·2003-01-00 ·Pages 287-90

Cellek S

Abstract

The effects of Y-27632, a Rho-kinase inhibitor and BAY41-2272, a soluble guanylyl cyclase activator, on the tone and nitrergic responses of rabbit vaginal wall and clitoral corpus cavernosum were investigated. Y-27632 and BAY41-2272 (10 nM-10 micro M) elicited concentration-dependent relaxation of phenylephrine-induced tone in both tissues. IC(50) values of Y-27632 for vaginal and clitoral tissues were 370+/-30 nM, and 467+/-14 nM, respectively. BAY41-2272 had IC(50) values of 478+/-54 nM and 304+/-38 nM respectively. The effect of the Y-27632 on the tissue tone was not affected by an inhibitor of nitric oxide synthase (L-NAME; 500 micro M). However, L-NAME reduced the potency of BAY41-2272 in the clitoral corpus cavernosum but not in the vaginal wall. BAY41-2272 enhanced nitrergic relaxation responses only in the clitoral corpus cavernosum. Y-27632 had no effect on nitrergic relaxations in either tissue. These results demonstrate that Y-27632 and BAY41-2272 elicit relaxation of the rabbit vaginal wall and clitoral corpus cavernosum.

MeSH Terms
Amides/pharmacology Animals Clitoris/drug effects,enzymology Dose-Response Relationship, Drug Enzyme Activation/drug effects,physiology Enzyme Inhibitors/pharmacology Female Guanylate Cyclase In Vitro Techniques Intracellular Signaling Peptides and Proteins Muscle Relaxation/drug effects,physiology Protein Serine-Threonine Kinases/antagonists & inhibitors,metabolism Pyrazoles/pharmacology Pyridines/pharmacology Rabbits Receptors, Cytoplasmic and Nuclear/metabolism Soluble Guanylyl Cyclase Vagina/drug effects,enzymology rho-Associated Kinases
Chemicals
3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo(3,4-b)pyridine Amides Enzyme Inhibitors Intracellular Signaling Peptides and Proteins Pyrazoles Pyridines Receptors, Cytoplasmic and Nuclear Y 27632 Protein Serine-Threonine Kinases rho-Associated Kinases Guanylate Cyclase Soluble Guanylyl Cyclase
Authors & Affiliations
1 authors, click to expand affiliations / ORCID
Cellek Selim
Wolfson Institute for Biomedical Research, University College London, Gower Street, Cruciform Building, London WC1E 6BT. s.cellek@ucl.ac.uk
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Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
Published
2003-01-00
Pages
287-90
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1573674
Subset
IM
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