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内皮素(Endothelin,ET)是血管内皮细胞分泌的迄今所知体内最强的缩血管多肽,参与高血压和心肌缺血等多种心血管疾病的发病过程。探寻有效的内皮素拮抗剂是当前急待解决的前沿课题。日本学者Ihara最近(1992)合成一种环五肽(-D-Asp-L-Pro-D-Val-L-Leu-D-Trp-),命名为BO 123。他们在大鼠血管平滑肌细胞(VSMC)上发现其特异拮抗~(125)I-ET1的结合,提示这种物质可能是ET_A受体特殊拮抗剂,但其生物学效应尚不了解。我们在大鼠整体、离体和
Endothelin (ET) is the strongest vasoconstrictor peptide secreted by vascular endothelial cells so far known, and is involved in the pathogenesis of many cardiovascular diseases such as hypertension and myocardial ischemia. The search for a valid endothelin antagonist is an urgent frontier issue to be solved urgently. Japanese scholar Ihara recently synthesized a cyclic pentapeptide (-D-Asp-L-Pro-D-Val-L-Leu-D-Trp-) named BO 123. Their specific antagonism of ~ (125) I-ET1 binding on rat vascular smooth muscle cells (VSMCs) suggests that this substance may be a specific antagonist of ET_A receptors but their biological effects are not yet known. We are whole, ex vivo and in rats