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缓激肽(BK)具有强烈的扩张小动脉、增加血管通透性、诱发疼痛以及使血管内皮细胞释放前列腺素的作用,这种体内的肽类物质与炎症等多种病理生理过程有关。 BK拮抗剂是将BK的部分氨基酸置换后合成的多肽物质.如将BK7位的脯氨酸用D-苯丙氨酸置换后,即为BK拮抗剂。进而将第5、8位的氨基酸用β-(2-噻嗯)-L-丙氨酸置换后(即A-BK_1),其与受体的亲和性明显增强。离体豚鼠回肠收缩试验表明,其pA_2值为5.3,以大鼠大网膜内注入BK
Bradykinin (BK) has a strong dilatation of arterioles, increase vascular permeability, induce pain and make the release of prostaglandins vascular endothelial cells, the body of the peptide substances and inflammation and other pathophysiological processes. The BK antagonist is a polypeptide material synthesized after partial amino acid replacement of BK, which is a BK antagonist after substitution of proline at position BK7 with D-phenylalanine. Furthermore, the amino acids at positions 5 and 8 were replaced with β- (2-thienyl) -L-alanine (ie, A-BK_1), and their affinity to the receptor was significantly enhanced. Isolated guinea pig ileum contraction test showed that its pA_2 value of 5.3, the rat omentum into the BK