Document Detail


Cicletanine-induced decreases in cytosolic Ca2+ level and contraction in vascular smooth muscle.
MedLine Citation:
PMID:  9517405     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The mechanism by which cicletanine (3-(4-chlorophenyl)-1,3-dihydro-7-hydroxy-6-methylfuro-[3,4-c]pyri dine) induces vasodilatation was examined in isolated vascular smooth muscle. Cicletanine inhibited the contraction induced by high K+, norepinephrine (NE) and prostaglandin F2alpha in a concentration-dependent manner in rat aorta. High K+ (15.8-72.7 mM) elicited elevation of cytosolic Ca2+ level ([Ca2+]i) and contraction in a concentration-dependent manner. Cicletanine (300 microM) inhibited the high K+-induced contractions without changing the [Ca2+]i/tension relationship. NE (3-300 nM) elicited greater contractions than high K+ at a given [Ca2+]i, suggesting that NE increased Ca2+ sensitivity of the contractile elements. Cicletanine inhibited the NE-induced contractions without changing the slope of the [Ca2+]i/tension relationship. Cicletanine inhibited the transient increases in both [Ca2+]i and muscle tension elicited by NE but not the transient increase in [Ca2+]i elicited by caffeine in Ca2+-free solution. Cicletanine did not inhibit contraction induced by Ca2+ in the permeabilized rabbit mesenteric artery with alpha-toxin. These results suggest that cicletanine inhibits vascular smooth muscle contraction by multiple mechanisms: 1) inhibition of Ca2+ influx via voltage-dependent Ca2+ channel and 2) inhibition of Ca2+ release mediated by the alpha-adrenoceptors, but not by caffeine.
Authors:
M Izumi; M Mitsui-Saito; H Ozaki; H Karaki
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Japanese journal of pharmacology     Volume:  76     ISSN:  0021-5198     ISO Abbreviation:  Jpn. J. Pharmacol.     Publication Date:  1998 Jan 
Date Detail:
Created Date:  1998-05-12     Completed Date:  1998-05-12     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  2983305R     Medline TA:  Jpn J Pharmacol     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  57-63     Citation Subset:  IM    
Affiliation:
Department of Veterinary Pharmacology, Graduate School of Agriculture and Life Sciences, The University of Tokyo, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antihypertensive Agents / pharmacology*
Aorta, Thoracic / drug effects,  metabolism
Caffeine / pharmacology
Calcium / antagonists & inhibitors,  metabolism*
Central Nervous System Stimulants / pharmacology
Cyclic GMP / analysis
Cytosol / drug effects*,  metabolism
Dinoprost
Dose-Response Relationship, Drug
Male
Muscle Contraction / drug effects
Muscle, Smooth, Vascular / drug effects*
Norepinephrine
Potassium Chloride
Pyridines / pharmacology*
Rabbits
Rats
Rats, Wistar
Receptors, Adrenergic, alpha / drug effects,  metabolism
Vasodilation / drug effects*
Chemical
Reg. No./Substance:
0/Antihypertensive Agents; 0/Central Nervous System Stimulants; 0/Pyridines; 0/Receptors, Adrenergic, alpha; 51-41-2/Norepinephrine; 551-11-1/Dinoprost; 58-08-2/Caffeine; 7440-70-2/Calcium; 7447-40-7/Potassium Chloride; 7665-99-8/Cyclic GMP; 87520-10-3/cycletanide

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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