Yoshida M, Latifpour J, Weiss R M
Section of Urology, Yale University School of Medicine, New Haven, Conn. 06510.
Dev Pharmacol Ther. 1992;18(1-2):100-7.
(+)-[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.
研究了(+)-[³H]PN 200-110(一种二氢吡啶类钙通道拮抗剂)在1日龄(新生)、6周龄(早产)、6月龄(幼年)和4.5至5岁(成年)雌性兔输尿管中的结合位点。(+)-[³H]PN 200-110与输尿管膜微粒的特异性结合具有饱和性、可逆性且亲和力高。在1日龄、6周龄、6月龄和4.5至5岁兔输尿管中,(+)-[³H]PN 200-110结合位点的密度(Bmax)分别为46.7±2.5、22.6±2.0、12.7±1.8和11.9±1.6 fmol/mg蛋白。所有组中(+)-[³H]PN 200-110结合位点的亲和常数(KD)相似。钙激动剂和拮抗剂抑制(+)-[³H]PN 200-110与1日龄和6周龄兔输尿管的结合,其Ki值的顺序如下:尼群地平<硝苯地平<BAY K 8644<维拉帕米。新生组和早产组之间的Ki值无显著差异。数据表明兔输尿管膜微粒中存在与年龄相关的(+)-[³H]PN 200-110结合位点下调。