Nilsson S, Leander S, Vallgren S, Håkanson R
Eur J Pharmacol. 1983 Jun 3;90(2-3):245-50. doi: 10.1016/0014-2999(83)90244-3.
Gastrins and cholecystokinins contract the isolated taenia coli of the guinea-pig. Porcine CCK-39 produced the greatest contractile response and human gastrin-17 I and -34 the weakest. Pentagastrin had the highest affinity to the receptors and non-sulphated CCK-8 the lowest. The contractions produced by the CCK peptides were reduced by the neuronal blocker tetrodotoxin and by the muscarinic blocker atropine but not by the substance P antagonist [D-Pro2,D-Trp7,9]SP. It is concluded that gastrin/CCK peptides act directly on smooth muscle cells and that in addition these peptides, notably sulphated forms of CCK, are capable of exciting cholinergic neurons (but not SP neurons) to cause smooth muscle contraction.
胃泌素和缩胆囊素可使豚鼠离体结肠带收缩。猪CCK - 39产生的收缩反应最大,而人胃泌素 - 17 I和 - 34产生的收缩反应最弱。五肽胃泌素对受体的亲和力最高,非硫酸化CCK - 8对受体的亲和力最低。CCK肽产生的收缩反应可被神经元阻滞剂河豚毒素和毒蕈碱阻滞剂阿托品减弱,但不能被P物质拮抗剂[D - Pro2,D - Trp7,9]SP减弱。由此得出结论,胃泌素/CCK肽直接作用于平滑肌细胞,此外,这些肽,尤其是硫酸化形式的CCK,能够刺激胆碱能神经元(而非P物质神经元)引起平滑肌收缩。