Literature DB >> 6975144

Bepridil (CERM-1978) an verapamil depression of contractions of rabbit aortic rings.

S Mras, N Sperelakis.   

Abstract

Isolated rings (about 1 mm wide) of rabbit ascending aorta were stimulated to contract by norepinephrine (NE), increased extracellular potassium ion concentration, or electrical stimulation. When tested 20 min after addition, bepridil (CERM-1978) (10(-5)-10(-6) M), a new antianginal agent, and verapamil (10(-5)-10(-6) M) depressed the contractile responses to high K+ (30 mM) and NE (10(-6) M). Bepridil was almost as potent as verapamil in this action. Responses to strong electrical field stimulation were not affected by either agent. The depressed responses to NE in Ca-free EGTA-containing solutions were not further affected by bepridil or verapamil. Contractile responses to NE obtained from depolarized tissues, however, were markedly depressed by bepridil. These results suggest that bepridil, like verapamil, acts to inhibit contractions of vascular smooth muscle by decreasing influx of extracellular Ca++. In depolarized vascular smooth muscle, bepridil may also exert an effect to depress contractions supported by intracellular Ca++ release.

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Year:  1981        PMID: 6975144     DOI: 10.1159/000158354

Source DB:  PubMed          Journal:  Blood Vessels        ISSN: 0303-6847


  5 in total

1.  Dependency of detrusor contractions on calcium sensitization and calcium entry through LOE-908-sensitive channels.

Authors:  J R Jezior; J D Brady; D I Rosenstein; K A McCammon; A S Miner; P H Ratz
Journal:  Br J Pharmacol       Date:  2001-09       Impact factor: 8.739

Review 2.  Calcium antagonists. Pharmacodynamic effects and mechanism of action.

Authors:  T T Zsotér; J G Church
Journal:  Drugs       Date:  1983-02       Impact factor: 9.546

3.  Regional differences in the actions of verapamil and isosorbide dinitrate on rabbit and dog vascular smooth muscle.

Authors:  S Ishikawa; H Izumi; S Satoh; Y Kanmura; T Itoh
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-12       Impact factor: 3.000

4.  Effects of calcium antagonistic drugs on the electrical activity of rabbit sino-atrial node.

Authors:  P A Molyvdas; N Sperelakis
Journal:  Br J Pharmacol       Date:  1986-05       Impact factor: 8.739

Review 5.  Bepridil: a pharmacological reappraisal of its potential beneficial effects in angina and tissue protection following ischemia.

Authors:  R Massingham; P A Van Zwieten
Journal:  Cardiovasc Drugs Ther       Date:  1989-10       Impact factor: 3.727

  5 in total

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