Bhattacharjee M, Chakraborty T, Banerjee R K
Department of Physiology, Indian Institute of Chemical Biology, Calcutta.
Biochem Pharmacol. 1990 Sep 1;40(5):1095-101. doi: 10.1016/0006-2952(90)90498-a.
Mercaptomethylimidazole (MMI), a potent antithyroid drug of the thionamide group, induces both acid and pepsinogen secretion independently in control and pylorus ligated mice. The effect is dose dependent and the drug is more effective than histamine, carbachol or isoproterenol when administered by an intraperitoneal route. MMI-stimulated pepsinogen secretion could be dissociated from the acid secretion by the use of cimetidine and omeprazole which effectively block the acid secretion without affecting the pepsinogen output. Neither acid nor pepsinogen secretion by MMI is inhibited by atropine indicating a lack of muscarinic receptor involvement in both of the processes. Nifedipine and verapamil, the calcium antagonists, by inhibiting the MMI-induced acid secretion can also dissociate pepsinogen secretion from the acid secretion. Clonidine, an alpha 2-agonist, and hexobarbital, a membrane active barbiturate, also inhibit acid secretion without affecting the pepsinogen output. These data indicate that MMI induces pepsinogen secretion independent of acid secretion. Furthermore, MMI-stimulated acid secretion is not additive with that of the histamine indicating same site (H2-receptor) of action while its synergistic effect in presence of carbachol (muscarinic receptor) indicates different site of interaction of the two compounds. On the other hand, an additive effect of MMI and carbachol on pepsinogen secretion indicates that while the carbachol effect is mediated through the muscarinic receptor, MMI stimulates pepsinogen secretion through some still unknown mechanism.
甲巯基甲基咪唑(MMI)是一种强效的硫代酰胺类抗甲状腺药物,在正常小鼠和幽门结扎小鼠中均可独立诱导胃酸和胃蛋白酶原分泌。该作用呈剂量依赖性,经腹腔给药时,该药物比组胺、卡巴胆碱或异丙肾上腺素更有效。使用西咪替丁和奥美拉唑可使MMI刺激的胃蛋白酶原分泌与胃酸分泌分离,这两种药物可有效阻断胃酸分泌,而不影响胃蛋白酶原的分泌量。阿托品对MMI诱导的胃酸和胃蛋白酶原分泌均无抑制作用,表明这两个过程均未涉及毒蕈碱受体。钙拮抗剂硝苯地平和维拉帕米通过抑制MMI诱导的胃酸分泌,也可使胃蛋白酶原分泌与胃酸分泌分离。α2激动剂可乐定和具有膜活性的巴比妥类药物己巴比妥也可抑制胃酸分泌,而不影响胃蛋白酶原的分泌量。这些数据表明,MMI诱导胃蛋白酶原分泌独立于胃酸分泌。此外,MMI刺激的胃酸分泌与组胺刺激的胃酸分泌无相加作用,表明二者作用于同一部位(H2受体),而在卡巴胆碱(毒蕈碱受体)存在时其具有协同作用,表明这两种化合物的相互作用部位不同。另一方面,MMI和卡巴胆碱对胃蛋白酶原分泌具有相加作用,这表明虽然卡巴胆碱的作用是通过毒蕈碱受体介导的,但MMI通过某种尚不清楚的机制刺激胃蛋白酶原分泌。