Forichon J, Couture E, Chayvialle J A, Minaire Y
INSERM U45, Hôpital E. Herriot, Lyon, France.
Eur J Clin Pharmacol. 1987;33(5):479-82. doi: 10.1007/BF00544239.
40749 RP, a pyridyl-2-tetrahydrothiophene derivative, is known to be a potent inhibitor of the gastric acid response to pentagastrin, betazole and a meal. In 6 healthy young volunteers, a single oral dose of 2 mg.kg-1 greatly reduced the gastric acid secretory response to sham-feeding. By contrast, neither gastric pepsin nor the plasma PP response were altered by the drug. No change was observed in plasma gastrin, motilin, VIP or somatostatin concentrations. The results show that 40749 RP is also active on the pure vagus-stimulated gastric acid secretion. The lack of effect upon gastric pepsin and plasma PP suggests that 40749 RP is not likely to act on the basolateral cholinergic receptor and that it affects further cellular steps involved in hydrogen ion secretion.
40749 RP是一种吡啶基-2-四氢噻吩衍生物,已知它是胃酸对五肽胃泌素、倍他唑和食物反应的强效抑制剂。在6名健康年轻志愿者中,单次口服剂量2mg·kg-1可显著降低假饲引起的胃酸分泌反应。相比之下,该药物对胃蛋白酶和血浆PP反应均无影响。血浆胃泌素、胃动素、血管活性肠肽或生长抑素浓度未见变化。结果表明,40749 RP对单纯迷走神经刺激的胃酸分泌也有作用。对胃蛋白酶和血浆PP无影响表明,40749 RP不太可能作用于基底外侧胆碱能受体,而是影响氢离子分泌所涉及的进一步细胞步骤。