新型阿朴长春胺酸衍生物VA-045对离体血管的作用：脑动脉选择性

Effects of VA-045, a novel apovincaminic acid derivative, on isolated blood vessels: cerebroarterial selectivity.

作者信息

Miyata N, Yamaura H, Tanaka M, Muramatsu M, Tsuchida K, Okuyama S, Otomo S

机构信息

Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

出版信息

Life Sci. 1993;52(18):PL181-6. doi: 10.1016/0024-3205(93)90115-j.

DOI:10.1016/0024-3205(93)90115-j

PMID:8387130

Abstract

We investigated the effects of VA-045, an apovincaminic acid derivative, on isolated blood vessels. VA-045 (10(-7)-10(-5) M) and vinpocetine (10(-7)-10(-5) M) inhibited the 64 mM KCl-induced and 10(-6)M norepinephrine (NE)-induced contraction of rat aortic strips. VA-045 (10(-7)-10(-4) M) and vinpocetine (10(-7)-10(-4) M) inhibited the activity of cyclic AMP and cyclic GMP phosphodiesterase in porcine coronary artery. VA-045 (3 x 10(-9-3 x 10(-6) M) relaxed the 64 mM KCl-induced contraction of the canine basilar artery without affecting the peripheral arteries. These results indicate that VA-045 selectively dilates canine cerebral artery, and that it may be a useful agent for the treatment of cerebrovascular diseases such as stroke.

摘要

我们研究了阿朴长春胺酸衍生物VA - 045对离体血管的作用。VA - 045（10⁻⁷ - 10⁻⁵M）和长春西汀（10⁻⁷ - 10⁻⁵M）抑制64 mM氯化钾诱导的以及10⁻⁶M去甲肾上腺素（NE）诱导的大鼠主动脉条收缩。VA - 045（10⁻⁷ - 10⁻⁴M）和长春西汀（10⁻⁷ - 10⁻⁴M）抑制猪冠状动脉中环磷酸腺苷（cAMP）和环磷酸鸟苷（cGMP）磷酸二酯酶的活性。VA - 045（3×10⁻⁹ - 3×10⁻⁶M）可舒张64 mM氯化钾诱导的犬基底动脉收缩，而不影响外周动脉。这些结果表明，VA - 045可选择性扩张犬脑动脉，可能是治疗中风等脑血管疾病的有效药物。