Basabe J C, Udrisar D P, Knopf C F, Aparicio N
Acta Diabetol Lat. 1977 Sep-Dec;14(5-6):263-72. doi: 10.1007/BF02580975.
Pharmacodynamic characteristics of pentoxyfylline (BL 191) related to insulin secretion by the isolated perfused rat pancreas are studied. The results obtained show that: 1) BL 191 (5 mM) is capable of stimulating insulin secretion, even in the presence of another stimulator; 2) BL 191 increases both phases of the secretion produced by constant arginine 20 mM/glucose 5 mM perfusion; 3) BL 191 significantly increases and turns biphasic the monophasic insulin secretion pattern produced by 1 microgram/ml glibenclamide; 4) the effects mentioned in points 2) and 3) are inhibited if the phosphodiesterase activator imidazole (300 mg/100 ml) is present in the perfusion medium; 5) the phosphodiesterase inhibitor theophylline has the same effects as BL 191, except for its inability to stimulate insulin release in the absence of another stimulator; 6) somatostatin (100 ng/ml) significantly inhibits insulin secretion produced by arginine/glucose or glibenclamide, as well as by arginine, glucose plus theophylline or BL 191, and by glibenclamide plus theophylline or BL 191, in both cases the inhibitory effect of somatostatin is reduced by the presence of BL 191 or theophylline.
研究了己酮可可碱(BL 191)与离体灌注大鼠胰腺胰岛素分泌相关的药效学特性。所得结果表明:1)即使存在另一种刺激剂,BL 191(5 mM)仍能够刺激胰岛素分泌;2)BL 191增加了由20 mM精氨酸/5 mM葡萄糖恒定灌注所产生的分泌的两个阶段;3)BL 191显著增加并使由1微克/毫升格列本脲产生的单相胰岛素分泌模式转变为双相;4)如果灌注介质中存在磷酸二酯酶激活剂咪唑(300毫克/100毫升),则第2点和第3点中提到的效应会受到抑制;5)磷酸二酯酶抑制剂茶碱具有与BL 191相同的效应,但在不存在另一种刺激剂时它无法刺激胰岛素释放;6)生长抑素(100纳克/毫升)显著抑制由精氨酸/葡萄糖或格列本脲产生的胰岛素分泌,以及由精氨酸、葡萄糖加茶碱或BL 191产生的胰岛素分泌,和由格列本脲加茶碱或BL 191产生的胰岛素分泌,在这两种情况下,生长抑素的抑制作用会因BL 191或茶碱的存在而降低。