苄普地尔（CERM - 1978）对兔主动脉环收缩的抑制作用与维拉帕米相似。（注：原英文句子表述不太完整准确，此译文是在尽量理解其含义基础上给出的较通顺版本）

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

作者信息

Mras S, Sperelakis N

出版信息

Blood Vessels. 1981;18(4-5):196-205. doi: 10.1159/000158354.

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.

摘要

兔升主动脉的孤立环（约1毫米宽）可被去甲肾上腺素（NE）、细胞外钾离子浓度升高或电刺激刺激收缩。在加入后20分钟进行测试时，新型抗心绞痛药物苄普地尔（CERM - 1978）（10⁻⁵ - 10⁻⁶ M）和维拉帕米（10⁻⁵ - 10⁻⁶ M）可抑制对高钾（30 mM）和NE（10⁻⁶ M）的收缩反应。苄普地尔在该作用中几乎与维拉帕米一样有效。两种药物均不影响对强电场刺激的反应。在不含钙的EGTA溶液中对NE的抑制反应不受苄普地尔或维拉帕米的进一步影响。然而，从去极化组织获得的对NE的收缩反应被苄普地尔显著抑制。这些结果表明，苄普地尔与维拉帕米一样，通过减少细胞外钙离子内流来抑制血管平滑肌收缩。在去极化的血管平滑肌中，苄普地尔也可能发挥作用，抑制由细胞内钙离子释放支持的收缩。