Abello J, Roche C, Cuber J C, Bernard C, Philippe J, Chayvialle J A
INSERM U45, Hôpital E. Herriot, Lyon France.
FEBS Lett. 1990 Sep 17;270(1-2):37-40. doi: 10.1016/0014-5793(90)81229-h.
The mechanisms of cholinergic stimulation of gastrin cells were studied in the rat pancreatic cell line B6 RIN. Carbachol induced an increase in intracellular Ca2+ and stimulated gastrin release in a dose-dependent manner over the range 10(-5)-10(-3) M. These effects were completely abolished by atropine, suggesting the implication of muscarinic cholinergic receptors. The binding properties of these receptors were investigated. [N-Methyl-3H]scopolamine [( 3H]NMS) binding on cell homogenates was time-dependent, saturable and consistent with a single high-affinity binding class (Kd = 39.5 pM, and Bmax = 7.9 fmol/mg DNA). Carbachol competitively inhibited [3H]NMS binding. The potency of inhibition of [3H]NMS binding by subtype selective antagonists was hexahydrodifenidol greater than pirenzepine greater than AF-DX 116. These results suggest the M3 muscarinic receptors may be involved in the carbachol-induced gastrin release from B6 RIN cells.
在大鼠胰腺细胞系B6 RIN中研究了胆碱能刺激胃泌素细胞的机制。卡巴胆碱诱导细胞内Ca2+增加,并在10(-5)-10(-3) M范围内以剂量依赖方式刺激胃泌素释放。这些效应被阿托品完全消除,提示毒蕈碱胆碱能受体参与其中。研究了这些受体的结合特性。[N-甲基-3H]东莨菪碱[(3H]NMS)与细胞匀浆的结合具有时间依赖性、饱和性,且符合单一高亲和力结合类别(Kd = 39.5 pM,Bmax = 7.9 fmol/mg DNA)。卡巴胆碱竞争性抑制[3H]NMS结合。亚型选择性拮抗剂对[3H]NMS结合的抑制效力为:六氢双苯丙醇大于哌仑西平大于AF-DX 116。这些结果提示M3毒蕈碱受体可能参与卡巴胆碱诱导的B6 RIN细胞胃泌素释放。