Petrillo M, Lazzaroni M, Fuccella L, Sassella D, Bianchi Porro G
Hepatogastroenterology. 1987 Jun;34(3):117-9.
MDL 646 is a 16-methyl-16-methoxy PGE analog with gastric antisecretory and cytoprotective activity in rats following oral administration. The efficacy of MDL 646 in inhibiting pentagastrin-stimulated acid secretion in man was investigated in a pilot crossover study in 10 male subjects given single oral doses of 500-1,000 mcg of the compound or placebo in randomized order. The doses showing consistent antisecretory effects in all subjects were 800 and 1,000 mcg, which caused a reduction in acid output of at least 25% over the whole test period (2.5 h), with greater inhibition in the first hour. The cytoprotective activity of MDL 646 was investigated by measuring the ability of single oral doses of 500 mcg of compound to prevent the drop in gastric potential difference (PD) induced by aspirin. The study was carried out in 8 male subjects given MDL 646 or placebo in randomized order in accordance with a single-blind crossover design. MDL 646 prevented the aspirin-induced drop in PD: No adverse reactions or changes in bowel habits were reported in either study. The compound is worth investigating further as a potential anti-ulcer agent.
MDL 646是一种16-甲基-16-甲氧基前列腺素E类似物，口服给药后在大鼠体内具有胃抗分泌和细胞保护活性。在一项初步交叉研究中，对10名男性受试者进行了MDL 646抑制人五肽胃泌素刺激胃酸分泌疗效的研究，受试者随机顺序单次口服500 - 1000微克该化合物或安慰剂。在所有受试者中显示出一致抗分泌作用的剂量为800微克和1000微克，在整个测试期（2.5小时）内导致胃酸分泌量减少至少25%，在第一小时内抑制作用更强。通过测量单次口服500微克化合物预防阿司匹林诱导的胃电位差（PD）下降的能力，研究了MDL 646的细胞保护活性。该研究按照单盲交叉设计，对8名男性受试者随机顺序给予MDL 646或安慰剂。MDL 646预防了阿司匹林诱导的PD下降：两项研究均未报告不良反应或排便习惯改变。作为一种潜在的抗溃疡药物，该化合物值得进一步研究。
