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EFFECTS OF CALMODULIN ANTAGONISTS ON TENSION AND CELLULAR CALCIUM CONTENT IN DEPOLARIZED VASCULAR AND INTESTINAL SMOOTH MUSCLES
- Source :
- British Journal of Pharmacology. 77:661-666
- Publication Year :
- 1982
- Publisher :
- Wiley, 1982.
-
Abstract
- 1 Several putative calmodulin antagonists have been examined for their inhibitory action on muscle tension and cellular Ca content in the K-depolarized vascular and intestinal smooth muscles. 2 The 65.4 mM K-induced sustained contraction in the media-intimal layer of rabbit aorta and the 45.4 mM K-induced sustained contraction in guinea-pig taenia coli were inhibited by the calmodulin antagonists, prenylamine, chlorpromazine, N2-dansyl-L-arginine-4-t-butylpiperadine amide (No. 233), and N-(6-aminohexyl)-5-chloro-1-naphthalenesulphonamide (W-7), and also by the organic Ca antagonists, verapamil and diltiazem. 3 The cellular Ca content in rabbit aorta and guinea-pig taenia coli as measured by a modified lanthanum technique increased in the high-K solutions. The increments were inhibited by these antagonists at concentrations similar to those required to inhibit the K-induced contractions. However, W-7 did not change (in aorta) or only slightly decreased (in taenia coli) the K-induced increase in the cellular Ca content. 4 A high concentration (2 X 10(-4)M) of W-7 increased the resting cellular Ca content without increasing the muscle tension in aorta. The increment was inhibited by verapamil, sodium nitroprusside or hypoxia (N2 aeration). 5 It is suggested that the inhibitory effects of prenylamine, chlorpromazine and No. 233 may be attributed mainly to the Ca antagonistic effect whereas W-7 may inhibit the process beyond the transmembrane Ca influx.
- Subjects :
- Male
medicine.medical_specialty
Calmodulin
chemistry.chemical_element
Aorta, Thoracic
In Vitro Techniques
Calcium
Muscle, Smooth, Vascular
Prenylamine
Internal medicine
Muscle tension
medicine
Animals
Diltiazem
Pharmacology
biology
Chemistry
Calcium-Binding Proteins
Muscle, Smooth
Taenia coli
Intestines
Endocrinology
medicine.anatomical_structure
Potassium
biology.protein
Verapamil
Rabbits
medicine.symptom
Muscle Contraction
Research Article
Muscle contraction
medicine.drug
Subjects
Details
- ISSN :
- 00071188
- Volume :
- 77
- Database :
- OpenAIRE
- Journal :
- British Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....6b8b5c8b3180e260b3b89d92b238128d