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溴化双氯酚(2-(3,4-二氯苯胺基)喹啉鎓溴化物)药理学的某些方面。第二部分:胃酸分泌抑制和抗溃疡作用。

Some aspects in the pharmacology of diclonium bromide (2-(3,4-dicholoroanilino)quinolizinium bromide). Part II: Gastric acid-antisecretory and antiulcerogenic actions.

作者信息

Goldenberg M M

出版信息

Arzneimittelforschung. 1976;26(3):347-50.

PMID:989324
Abstract

Diconium bromide, 2-(3,4-dichloroanilino)-quinolizinium bromide, a potent antispasmodic in the lower bowel of the dog, was found in the present study to exert gastric acid-antisecretory and antiulcerogenic activities in the rat stomach. These effects were demonstrated by means of short- and long-term pyloric ligation, acetylsalicylic acid (ASA)-induced ulcerogenesis, and cold-and-restraint stress studies. A reduction of gastric acid concentration by the drug was probably responsible for the decrease in the degree of ulceration and hemorrhagic lesion formation. The drug's inhibition of stress hemorrhagic lesions may be related to an effect both on gastric HCl secretion and on the vasculature in the glabdular mucosa. The delay of gastric emptying by diclonium bromide results from its known antispasmodic or smooth-muscle depressant action. The toxicity of diclonium bromide, perorally, was low in rats and overt signs of drug effect were not evident until toxic doses were administered. It is concluded that diclonium bromide may represent a useful non-anticholinergic drug effective in treating both peptic ulcers and spasticity of the colon (irritable-colon syndrome) in man.

摘要

二溴地可铵,即2-(3,4-二氯苯胺基)-喹嗪鎓溴化物,在犬的下消化道中是一种有效的解痉剂,在本研究中发现它在大鼠胃中具有胃酸分泌抑制和抗溃疡活性。这些作用通过短期和长期幽门结扎、乙酰水杨酸(ASA)诱导的溃疡形成以及寒冷和束缚应激研究得以证明。药物使胃酸浓度降低可能是溃疡程度和出血性病变形成减少的原因。药物对应激性出血性病变的抑制作用可能与对胃盐酸分泌和腺性黏膜血管系统的作用有关。二溴地可铵导致胃排空延迟是由于其已知的解痉或平滑肌抑制作用。二溴地可铵经口给药在大鼠中的毒性较低,直到给予中毒剂量才出现明显的药物作用迹象。结论是,二溴地可铵可能是一种有用的非抗胆碱能药物,对治疗人类消化性溃疡和结肠痉挛(肠易激综合征)有效。

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