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钙拮抗剂Wy-47,037对大鼠应激性溃疡的保护作用。

Protection by the calcium antagonist Wy-47,037 against stress ulceration in the rat.

作者信息

Nielsen S T, Sulkowski T S

机构信息

Department of Experimental Therapeutics, Wyeth Laboratories, Inc., Philadelphia, PA 19101.

出版信息

Pharmacol Biochem Behav. 1988 Jan;29(1):129-32. doi: 10.1016/0091-3057(88)90285-7.

Abstract

Wy-47,037, a novel compound with both intracellular and extracellular calcium-blocking properties, was evaluated for its effects on cold/restraint stress induced ulceration in the rat. Wy-47,037 dose-dependently inhibited ulcerogenesis; with an ED50 of 8 mg/kg, PO, it was approximately twice as potent as nitrendipine (ED50 = 15 mg/kg). Wy-47,037 also reduced basal gastric acid secretion (ED50 = 7 mg/kg) and gastrointestinal motility (ED50 = 16 mg/kg). It is thus possible that Wy-47,037's alteration of basal gastric acid secretion and/or of gastrointestinal motility may contribute to its therapeutic efficacy against stress induced ulcer formation.

摘要

Wy-47037是一种兼具细胞内和细胞外钙阻断特性的新型化合物,对其在大鼠冷/束缚应激诱导溃疡形成方面的作用进行了评估。Wy-47037剂量依赖性地抑制溃疡形成;口服时ED50为8mg/kg,其效力约为尼群地平(ED50 = 15mg/kg)的两倍。Wy-47037还可降低基础胃酸分泌(ED50 = 7mg/kg)和胃肠蠕动(ED50 = 16mg/kg)。因此,Wy-47037对基础胃酸分泌和/或胃肠蠕动的改变可能有助于其对应激诱导溃疡形成的治疗效果。

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