兔输尿管钙拮抗剂受体的年龄相关性变化。

M. Yoshida, J. Latifpour, R. Weiss
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引用次数: 7

摘要

(+)-[3H]PN 200-110(一种二氢吡啶钙通道拮抗剂)结合位点在1天(新生儿)、6周(早产儿)、6个月(幼兔)和4.5- 5岁(大兔)母兔输尿管中进行了研究。(+)-[3H]PN 200-110与输尿管膜颗粒的特异性结合是饱和、可逆和高亲和力的。(+)-[3H]PN 200-110结合位点在1天、6周、6个月和4.5 ~ 5年的兔输尿管中的蛋白质密度(Bmax)分别为46.7 +/- 2.5、22.6 +/- 2.0、12.7 +/- 1.8和11.9 +/- 1.6 fmol/mg。(+)-[3H]PN 200-110结合位点的亲和常数(KD)在所有组中相似。钙激动剂和拮抗剂抑制(+)-[3H]PN 200-110与1天和6周家兔输尿管的结合,Ki值的大小顺序为:尼群地平<硝苯地平< BAY k8644 <维拉帕米。新生儿组和早产儿组间Ki值无显著差异。数据表明,兔输尿管膜颗粒中(+)-[3H]PN 200-110结合位点存在与年龄相关的下调。
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Age-related changes in calcium antagonist receptors in rabbit ureter.
(+)-[3H]PN 200-110 (a dihydropyridine calcium channel antagonist) binding sites were studied in ureters of 1-day (neonatal), 6-week (premature), 6-month (young) and 4.5- to 5-year (old) female rabbits. Specific binding of (+)-[3H]PN 200-110 to ureteral membrane particulates was saturable, reversible and of high affinity. The densities (Bmax) of (+)-[3H]PN 200-110 binding sites were 46.7 +/- 2.5, 22.6 +/- 2.0, 12.7 +/- 1.8 and 11.9 +/- 1.6 fmol/mg protein in 1-day, 6-week, 6-month and 4.5- to 5-year rabbit ureters, respectively. The affinity constants (KD) of the binding sites for (+)-[3H]PN 200-110 were similar in all groups. Calcium agonists and antagonists inhibited (+)-[3H]PN 200-110 binding to 1-day and 6-week rabbit ureters with the following rank order of Ki values: nitrendipine < nifedipine < BAY K 8644 < verapamil. There were no significant differences in Ki values between the neonatal and premature groups. The data demonstrate the presence of an age-related down-regulation of (+)-[3H]PN 200-110 binding sites in rabbit ureteral membrane particulates.
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