Johannesson N, Andersson K E, Joelsson B, Persson C G
Am Rev Respir Dis. 1985 Jan;131(1):26-30. doi: 10.1164/arrd.1985.131.1.26.
The study was designed to obtain information on selected extrapulmonary effects of enprofylline, an adenosine-non-blocking alkylxanthine that is about 5 times more potent as a bronchodilator than the adenosine receptor antagonist theophylline. Effects of theophylline (5.0 mg/kg) on lower esophageal sphincter pressure (LESP), gastric secretion, and diuresis and of enprofylline (1.5 mg/kg intravenously producing about 2 micrograms/ml plasma) were examined in 8 healthy volunteers. Enprofylline and theophylline decreased LESP (by 5.0 +/- 2.6 mm Hg, mean +/- SD, p less than 0.001, and by 5.8 +/- 2.7 mmHg, p less than 0.001, respectively), but only theophylline stimulated gastric secretion (volume p less than 0.01 and acidity p less than 0.01) and urine production (volume p less than 0.01 and sodium chloride excretion p less than 0.01). Neither xanthine affected plasma gastrin. Enprofylline and theophylline can be expected to have a similar ability to reduce the barrier to gastroesophageal reflux, but only the latter would have additional stimulant effects on gastric secretion and diuresis. These findings may have clinical significance and suggest a role for adenosine in regulating gastric secretion (and diuresis) but not LESP.
本研究旨在获取有关恩丙茶碱（一种非腺苷阻断性烷基黄嘌呤，作为支气管扩张剂，其效力约为腺苷受体拮抗剂茶碱的5倍）特定肺外效应的信息。在8名健康志愿者中，研究了茶碱（5.0毫克/千克）对食管下括约肌压力（LESP）、胃液分泌和利尿的影响，以及恩丙茶碱（静脉注射1.5毫克/千克，产生约2微克/毫升血浆浓度）的影响。恩丙茶碱和茶碱均降低了LESP（分别降低5.0±2.6毫米汞柱，平均值±标准差，p<0.001，以及5.8±2.7毫米汞柱，p<0.001），但只有茶碱刺激了胃液分泌（量p<0.01，酸度p<0.01）和尿液生成（量p<0.01，氯化钠排泄p<0.01）。两种黄嘌呤均未影响血浆胃泌素。预计恩丙茶碱和茶碱降低胃食管反流屏障的能力相似，但只有后者会对胃液分泌和利尿产生额外的刺激作用。这些发现可能具有临床意义，并提示腺苷在调节胃液分泌（和利尿）而非LESP方面发挥作用。
