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新型GABA模拟剂N-邻苯二甲酰基GABA的抗溃疡活性

Antiulcer activity of N-phthaloyl GABA--a new GABA mimetic agent.

作者信息

Bhowmick S, Bose R, Pal M, Pal S P

机构信息

Department of Pharmacy, Jadavpur University, Calcutta, India.

出版信息

Indian J Exp Biol. 1990 Feb;28(2):190-2.

PMID:2115022
Abstract

N-phthaloyl GABA (P. GABA) inhibited gastric ulceration induced by 3 hr restraint stress at 4 degrees C (CRS) in albino rats. Antiulcer activity of P. GABA was compared with sodium valproate and cimetidine. P. GABA, sodium valproate and cimetidine showed a dose dependent reduction of gastric ulceration. Pretreatment with GABA antagonists-bicuculline methiodide (0.5 mg/kg, im) or 3 mercaptopropionic acid (2 mg/kg, im) reversed the antiulcerogenic activity of both the drugs (P. GABA and sodium valproate). GABA antagonists as such did not induce gastric ulceration in normal rats.

摘要

N-邻苯二甲酰基γ-氨基丁酸(P. GABA)可抑制白化大鼠在4℃下3小时束缚应激(CRS)诱导的胃溃疡形成。将P. GABA的抗溃疡活性与丙戊酸钠和西咪替丁进行了比较。P. GABA、丙戊酸钠和西咪替丁均呈剂量依赖性地减轻胃溃疡。用GABA拮抗剂——碘化荷包牡丹碱(0.5毫克/千克,腹腔注射)或3-巯基丙酸(2毫克/千克,腹腔注射)预处理可逆转这两种药物(P. GABA和丙戊酸钠)的抗溃疡活性。GABA拮抗剂本身不会在正常大鼠中诱导胃溃疡形成。

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