Harty R F, Maico D G, McGuigan J E
Department of Internal Medicine, University of Nebraska Medical Center, Omaha 68105.
Peptides. 1988 May-Jun;9(3):463-8. doi: 10.1016/0196-9781(88)90148-9.
Rat antral mucosal fragments were maintained in short-term culture to examine the relative potencies and receptor specificity of the cholinergic agonist, carbachol, and adrenergic agents, norepinephrine, isoproterenol, clonidine and phenylephrine in stimulating gastrin release. Results of these studies indicate that norepinephrine and carbachol evoke pharmacologically and temporally distinctive patterns of antral gastrin release. Dose-response experiments indicate that norepinephrine is approximately 10,000 times more potent on a molar basis than carbachol in stimulating antral gastrin release. Adrenergic (norepinephrine, isoproterenol) stimulation of antral gastrin release was prevented by propranolol, and cholinergic- (carbachol) mediated peptide release was blocked by both atropine and pirenzepine. Phenylephrine and clonidine did not alter basal gastrin release. The pattern of peptide release as a function of time was quite different for each agent: norepinephrine exerted its stimulatory effect acutely during the initial 30 minutes of incubation, while carbachol exhibited a sustained stimulatory action throughout the 2-hour culture period. In conclusion, data from these studies suggests that there are marked differences between norepinephrine and carbachol in their pharmacological potency and time-dependent activation of the G cell.
将大鼠胃窦黏膜碎片进行短期培养，以检测胆碱能激动剂卡巴胆碱以及肾上腺素能药物去甲肾上腺素、异丙肾上腺素、可乐定和去氧肾上腺素在刺激胃泌素释放方面的相对效力和受体特异性。这些研究结果表明，去甲肾上腺素和卡巴胆碱引起胃窦胃泌素释放的药理学和时间模式不同。剂量反应实验表明，在刺激胃窦胃泌素释放方面，去甲肾上腺素的摩尔效力比卡巴胆碱强约10000倍。普萘洛尔可阻止肾上腺素能（去甲肾上腺素、异丙肾上腺素）对胃窦胃泌素释放的刺激，阿托品和哌仑西平均可阻断胆碱能（卡巴胆碱）介导的肽释放。去氧肾上腺素和可乐定不改变基础胃泌素释放。每种药物引起的肽释放随时间变化的模式差异很大：去甲肾上腺素在孵育最初30分钟内急性发挥刺激作用，而卡巴胆碱在整个2小时培养期内表现出持续的刺激作用。总之，这些研究数据表明，去甲肾上腺素和卡巴胆碱在药理效力和对G细胞的时间依赖性激活方面存在显著差异。
