Katsoulis S, Conlon J M
Clinical Research Group for Gastrointestinal Endocrinology, Max-Planck-Gesellschaft, University of Göttingen, F.R.G.
Eur J Pharmacol. 1989 Mar 14;162(1):129-34. doi: 10.1016/0014-2999(89)90612-2.
Rat and human alpha- and beta-calcitonin gene-related peptide (CGRP), in the concentration range 1-100 nM, produced sustained relaxations of longitudinal muscle from the rat fundus and guinea pig gastric corpus. The peptides were equipotent and equally effective. Tetrodotoxin, adrenoceptor and purine receptor antagonists, somatostatin, apamin and Tyr-rat alpha-CGRP-(28-37) peptide did not modify the action of the CGRP peptides. The CGRP-induced responses were inhibited by verapamil and potentiated by Bay K-8644. Incubation of the tissues with indomethacin markedly reduced the magnitude of the CGRP- and adrenaline-induced relaxations, but their responsiveness was restored by addition of prostaglandins E1, E2 and F2 alpha in concentrations that alone did not affect the motility of the indomethacin-treated strips. It is suggested that an inhibitory receptor for CGRP on gastric smooth muscle cells is linked to calcium channels and may be activated or sensitized by endogenous prostaglandins.
在1 - 100 nM的浓度范围内，大鼠和人类的α-及β-降钙素基因相关肽（CGRP）可使大鼠胃底和豚鼠胃体的纵行肌产生持续舒张。这些肽类具有同等效力且效果相同。河豚毒素、肾上腺素能受体和嘌呤受体拮抗剂、生长抑素、蜂毒明肽以及酪氨酸-大鼠α-CGRP-（28 - 37）肽均不改变CGRP肽的作用。CGRP诱导的反应可被维拉帕米抑制，并被Bay K - 8644增强。用吲哚美辛孵育组织可显著降低CGRP和肾上腺素诱导的舒张幅度，但通过添加单独不影响吲哚美辛处理条带运动性的前列腺素E1、E2和F2α可恢复其反应性。提示胃平滑肌细胞上CGRP的抑制性受体与钙通道相关，且可能被内源性前列腺素激活或致敏。
