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      Bepridil (CERM-1978) and Verapamil Depression of Contractions of Rabbit Aortic Rings

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          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<sup>–5</sup>–10<sup>-6</sup> M), a new antianginal agent, and verapamil (10<sup>-5</sup>–10<sup>–6</sup> M) depressed the contractile responses to high K<sup>+</sup> (30 mM) and NE (10<sup>-6</sup> 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 or 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<sup>++</sup>. In depolarized vascular smooth muscle, bepridil may also exert an effect to depress contractions supported by intracellular Ca<sup>++</sup> release.

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          Author and article information

          Journal
          JVR
          J Vasc Res
          10.1159/issn.1018-1172
          Journal of Vascular Research
          S. Karger AG
          1018-1172
          1423-0135
          1981
          1981
          19 September 2008
          : 18
          : 4-5
          : 196-205
          Affiliations
          Department of Physiology, University of Virginia School of Medicine, Charlottesville, Va., USA
          Article
          158354 Blood Vessels 1981;18:196–205
          10.1159/000158354
          © 1981 S. Karger AG, Basel

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          Page count
          Pages: 10
          Categories
          Research Paper

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