Roche S, Gusdinar T, Bali J P, Magous R
Laboratoire de Biochimie des Membranes, CNRS UPR-8402 - INSERM U-249, Faculté de Pharmacie, Montpellier, France.
Mol Cell Endocrinol. 1991 May;77(1-3):109-13. doi: 10.1016/0303-7207(91)90064-y.
The relationship between gastrin-stimulated inositol 1,4,5-trisphosphate (Ins(1,4,5)P3) content and [14C]aminopyrine ([14C]AP) uptake (an index of in vitro acid secretion) was investigated in a population of highly enriched rabbit parietal cells (90 +/- 5%). Gastrin induced a rapid rise in Ins(1,4,5)P3 content which was maximal within 15 s of stimulation (2- to 2.5-fold basal level) followed by a rapid decrease within 30 s; a high Ins(1,4,5)P3 level could also be observed after a longer time of hormone stimulation (180 s). Gastrin dose-dependently induced Ins(1,4,5)P3 accumulation and [14C]AP uptake; both dose-response curves were similar (EC50 approximately 0.1 nM). Furthermore, L-365,260 (3-(acylamino)benzodiazepine), a selective gastrin/CCK-B receptor antagonist, dose-dependently inhibited Ins(1,4,5)P3 production and [14C]AP accumulation induced by 10 nM gastrin with a similar potency (IC50 approximately 1-2 nM). These results led us to conclude that Ins(1,4,5)P3 is involved in gastrin-stimulated acid secretory activity of gastric parietal cells.
在一群高度富集的兔壁细胞（90±5%）中，研究了胃泌素刺激的肌醇1,4,5-三磷酸（Ins(1,4,5)P3）含量与[14C]氨基比林（[14C]AP）摄取（体外酸分泌指标）之间的关系。胃泌素诱导Ins(1,4,5)P3含量迅速升高，在刺激后15秒内达到最大值（基础水平的2至2.5倍），随后在30秒内迅速下降；在激素刺激较长时间（180秒）后也可观察到较高的Ins(1,4,5)P3水平。胃泌素剂量依赖性地诱导Ins(1,4,5)P3积累和[14C]AP摄取；两条剂量反应曲线相似（EC50约为0.1 nM）。此外，选择性胃泌素/CCK-B受体拮抗剂L-365,260（3-(酰基氨基)苯并二氮杂卓）剂量依赖性地抑制10 nM胃泌素诱导的Ins(1,4,5)P3产生和[14C]AP积累，效力相似（IC50约为1至2 nM）。这些结果使我们得出结论，Ins(1,4,5)P3参与胃壁细胞胃泌素刺激的酸分泌活性。
