Furuya M, Ohnuma N, Takehisa M, Hayashi Y, Ishihara T, Minamino N, Kangawa K, Matsuo H
Suntory Institute for Biomedical Research, Osaka, Japan.
Eur J Pharmacol. 1991 Aug 6;200(2-3):233-7. doi: 10.1016/0014-2999(91)90577-d.
The pharmacological activities of synthetic mammalian brain natriuretic peptides (BNP) from the human, pig and rat were examined in rats. These peptides all elicited diuresis and hypotension, relaxed isolated rat aorta, augmented cyclic GMP concentration in cultured rat vascular smooth muscle cells, and bound to the cells with a high affinity. Pig and rat BNPs were as active as atrial natriuretic peptides from the human and the rat (alpha-hANP and alpha-rANP) for the diuretic and hypotensive effects as well as for cyclic GMP augmentation, while human BNP was about 10 times less potent. Rat BNP was not as active as the other peptides in competing with the binding of [125I]alpha-hANP to rat vascular smooth muscle cells. Thus, the BNPs did not have identical pharmacological profiles although the potencies of the peptides for cyclic GMP augmentation correlated well to those for vasorelaxation.
在大鼠中检测了源自人、猪和大鼠的合成哺乳动物脑钠肽(BNP)的药理活性。这些肽均引起利尿和低血压,使离体大鼠主动脉舒张,增加培养的大鼠血管平滑肌细胞中环鸟苷酸(cGMP)浓度,并以高亲和力与细胞结合。猪和大鼠的BNP在利尿、降压作用以及cGMP增加方面与人及大鼠的心房钠尿肽(α-hANP和α-rANP)活性相当,而人BNP的效力约低10倍。在与[125I]α-hANP结合到大鼠血管平滑肌细胞的竞争中,大鼠BNP不如其他肽活跃。因此,尽管这些肽增加cGMP的效力与血管舒张的效力密切相关,但BNP并不具有相同的药理特征。