Schwartz G J, Moran T H, McHugh P R
Department of Psychiatry and Behavioral Sciences Johns Hopkins University School of Medicine, Baltimore, MD 21205.
Peptides. 1990 Nov-Dec;11(6):1199-203. doi: 10.1016/0196-9781(90)90152-u.
To determine the functional role for and the pharmacological specificity of developing gastrointestinal CCK receptors, in vitro pyloric contractility and autoradiographic CCK receptor binding were examined in pups aged 1-20 days. CCK contracted the gastroduodenal junction at all ages, while nonsulfated CCK-8 (d-CCK) was less potent. Autoradiographic studies revealed CCK binding localized to the gastroduodenal junction throughout development. MK-329, a specific type A CCK receptor antagonist, completely displaced 125I CCK-8 binding at all ages, while d-CCK displaced binding at ages at which d-CCK elicited gastroduodenal contractility. The results demonstrate a physiological role for and pharmacological specificity of neonatal gastroduodenal CCK receptors.
为了确定发育中的胃肠道CCK受体的功能作用和药理学特异性，对1至20日龄幼崽的体外幽门收缩性和放射自显影CCK受体结合进行了检测。CCK在所有年龄段均可使胃十二指肠连接处收缩，而非硫酸化CCK-8（d-CCK）的效力较低。放射自显影研究显示，在整个发育过程中，CCK结合定位于胃十二指肠连接处。特异性A类CCK受体拮抗剂MK-329在所有年龄段均可完全取代125I CCK-8结合，而d-CCK在其引起胃十二指肠收缩的年龄段可取代结合。结果证明了新生胃十二指肠CCK受体的生理作用和药理学特异性。
