Rosenberg V, Biezunski D, Gonda M, Dreiling D A, Rudick J, Robert A
Surgery. 1976 May;79(5):509-14.
Effects of a synthetic prostaglandin analog-16--16-dimethyl prostaglandin E2, methyl ester (16-diMe-PGE2)--on pancreatic secretion were evaluated in seven dogs with chronic duodenal fistulas. Graded doses of 16-diMe-PGE2 were administered intravenously (0.1, 0.3, 0.5, and 1.0 mug per kilogram, intraduodenally, or intragastrically (15, 30, 50, 100 mug per kilogram) with the pancreas in the resting state or in response to (1) secretin and (2) secretin with cholecystokinin-pancreozymin. Profound and prolonged inhibition of volume and bicarbonate concentration of secretion occurred in the resting and stimulated gland. ED50 was 0.31 mug per kilogram intravenously (1/75 the ED50 for PGE1) and 25 mug per kilogram intraduodenally. As with PGE1, stimulation of enzymes occurred, even with doses that were subthreshold for inhibition of volume and HCO3. Like PGE1, 16-diMe-PGE2 has a dual action on the intact canine pancreas (stimulation of enzymes and inhibition of volume and electrolytes), but is much more potent, has a prolonged action, and is active intraduodenally and intragastrically. Nonsteroid inhibitors of endogenous prostaglandin synthesis did not alter these effects.
在七只患有慢性十二指肠瘘的犬中评估了一种合成前列腺素类似物——16,16-二甲基前列腺素E2甲酯(16-二甲基-PGE2)对胰腺分泌的影响。分别在胰腺处于静息状态或对(1)促胰液素和(2)促胰液素加缩胆囊素-促胰酶素产生反应时,以静脉注射(每千克0.1、0.3、0.5和1.0微克)、十二指肠内注射或胃内注射(每千克15、30、50、100微克)的方式给予不同剂量的16-二甲基-PGE2。在静息和受刺激的腺体中,均出现了对分泌量和碳酸氢盐浓度的深刻且持久的抑制。静脉注射时的半数有效剂量(ED50)为每千克0.31微克(为PGE1的ED50的1/75),十二指肠内注射时为每千克25微克。与PGE1一样,即使是在抑制分泌量和HCO3的阈下剂量下,也会出现酶的分泌增加。与PGE1一样,16-二甲基-PGE2对完整的犬胰腺具有双重作用(刺激酶分泌以及抑制分泌量和电解质),但效力更强,作用持续时间更长,且在十二指肠内和胃内均有活性。内源性前列腺素合成的非甾体抑制剂并未改变这些作用。