Dajani E Z, Callison D A
Prostaglandins. 1976 May;11(5):799-808. doi: 10.1016/0090-6980(76)90188-x.
The gastric antisecretory actions of (15S)-15-methyl prostaglandin E2 methyl ester (Me-PGE2) and Prostaglandin E2 (PGE2) were evaluated in the unanesthetized gastric fistula rhesus monkey. Secretion was submaximally stimulated by multiple subcutaneous injections of histamine acid phosphate given every hour for four consecutive hours. When a steady-state plateau of gastric secretion was reached, the PG's were administered as a single bolus dose either intravenously (i.v.) or intragastrically (i.g.). Both PG's inhibited histamine-stimulated gastric secretion. The PG's showed greater sensitivity in inhibiting acid concentration while not affecting volume output. Active i.v. and i.g. antisecretory doses of ME-PGE2 ranged from 3 to 10 mug/kg, while PGE2 showed significant antisecretory activity at i.v. bolus doses of 30-100 mug/kg and i.g. bolus dose of 1.0 mg/kg. Thus, Me-PGE2 is estimated to be at least 10 and 300 times more potent than PGE2 by the i.v. and i.g. administration routes, respectively. These findings indicate that the rhesus monkey shows some similarities to man in responsiveness to gastric secretory inhibition by E-prostaglandins.
在未麻醉的胃瘘恒河猴中评估了(15S)-15-甲基前列腺素E2甲酯(Me-PGE2)和前列腺素E2(PGE2)的胃抗分泌作用。通过每小时皮下注射多次磷酸组胺连续4小时来亚最大程度地刺激分泌。当达到胃分泌的稳态平台时,将PG作为单次推注剂量静脉内(i.v.)或胃内(i.g.)给药。两种PG均抑制组胺刺激的胃分泌。PG在抑制酸浓度方面表现出更高的敏感性,而不影响容量输出。Me-PGE2的有效静脉内和胃内抗分泌剂量范围为3至10μg/kg,而PGE2在静脉推注剂量为30 - 100μg/kg和胃内推注剂量为1.0mg/kg时显示出显著的抗分泌活性。因此,通过静脉内和胃内给药途径,Me-PGE2的效力估计分别比PGE2至少高10倍和300倍。这些发现表明,恒河猴在对E-前列腺素抑制胃分泌的反应性方面与人有一些相似之处。