Glavin G B
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
Life Sci. 1995;56(18):PL365-8. doi: 10.1016/0024-3205(95)00118-p.
Dopaminergic compounds affect gastric secretion and response to experimental gastric mucosal injury. We showed previously that the novel dopamine D4 receptor antagonist, clozapine, significantly reduces gastric acid secretion and restraint stress-induced gastric lesions. Because the selectivity of clozapine for D4 receptors has recently been questioned, we tested the ability of a known D1 receptor blocker, SCH23390, to affect clozapine-induced reduction in gastric acid secretion. SCH23390 given i.p. or i.c.v., at doses that did not affect gastric acid secretion, significantly blocked the anti-secretory effect of clozapine, administered either peripherally or centrally. These data suggest that neither clozapine nor SCH23390 exhibit as high a degree of selectivity for the dopamine D4 and D1 receptor, respectively, as previously believed.
多巴胺能化合物会影响胃分泌及对实验性胃黏膜损伤的反应。我们之前表明，新型多巴胺D4受体拮抗剂氯氮平可显著减少胃酸分泌及束缚应激诱导的胃损伤。由于最近有人质疑氯氮平对D4受体的选择性，我们测试了一种已知的D1受体阻滞剂SCH23390影响氯氮平诱导的胃酸分泌减少的能力。腹腔注射或脑室内注射不影响胃酸分泌剂量的SCH23390，可显著阻断外周或中枢给予氯氮平的抗分泌作用。这些数据表明，氯氮平和SCH23390对多巴胺D4和D1受体的选择性程度均不如之前认为的那么高。
