Magous R, Bali J P
Eur J Pharmacol. 1982 Aug 13;82(1-2):47-54. doi: 10.1016/0014-2999(82)90551-9.
A biologically active gastrin analogue, 125I-HG-13, appears to bind specifically to saturable binding sites on isolated rabbit gastric mucosal cells: Kd = 70 pM at pH 7.4 and at 37 degrees C. Increasing incubation temperature from +4 degrees C to +37 degrees C increased specific binding. Gastrin binding was shown to be reversible and the dissociation rate was enhanced with cold gastrin. The binding sites were saturated with 0.2 fmol of labelled gastrin per 10(6) mucosal cells. Gastrin binding was not inhibited by secretin, glucagon, Met-enkephalin, physalaemin, eledoisin, BPP, VIP, carbachol, histamine, atropine or cimetidine. Gastrin analogues (HG-4, HG-8, (Leu15)-HG-17), CCK-7 and gastrin antagonists (proglumide or benzotript) inhibited 125I-HG-13 specific binding. We concluded that isolated cells from rabbit gastric fundic mucosa contain high-affinity binding sites for a gastrin analogue (Nle11)-HG-13.
一种具有生物活性的胃泌素类似物,125I-HG-13,似乎能特异性结合分离的兔胃黏膜细胞上的可饱和结合位点:在pH 7.4和37℃时,解离常数(Kd)为70皮摩尔。将孵育温度从4℃提高到37℃可增加特异性结合。胃泌素结合显示为可逆性,且冷胃泌素可增强解离速率。每10(6)个黏膜细胞用0.2飞摩尔标记胃泌素可使结合位点饱和。促胰液素、胰高血糖素、甲硫氨酸脑啡肽、蛙皮素、伊索肽、蛙皮素样肽、血管活性肠肽、卡巴胆碱、组胺、阿托品或西咪替丁均不抑制胃泌素结合。胃泌素类似物(HG-4、HG-8、(Leu15)-HG-17)、胆囊收缩素-7和胃泌素拮抗剂(丙谷胺或苯卓曲肽)可抑制125I-HG-13的特异性结合。我们得出结论,兔胃底黏膜的分离细胞含有一种胃泌素类似物(Nle11)-HG-13的高亲和力结合位点。