STIMULATION OF INSULIN-SECRETION AND IMPROVEMENT OF GLUCOSE-TOLERANCE IN RAT AND DOG BY THE P2Y-PURINOCEPTOR AGONIST, ADENOSINE-5'-O-(2-THIODIPHOSPHATE)
STIMULATION OF INSULIN-SECRETION AND IMPROVEMENT OF GLUCOSE-TOLERANCE IN RAT AND DOG BY THE P2Y-PURINOCEPTOR AGONIST, ADENOSINE-5'-O-(2-THIODIPHOSPHATE)
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DOI：
10.1111/j.1476-5381.1993.tb13551.x
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发表时间：
1993-05-01
影响因子：
7.3
通讯作者：
LOUBATIERESMARIANI, MM
中科院分区：
文献类型：
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作者：
HILLAIREBUYS, D;BERTRAND, G;LOUBATIERESMARIANI, MM
1研究了P2y-嘌呤受体激动剂腺苷-5‘-O-(2-硫代二磷酸)(ADPbetaS)对大鼠和犬胰岛素分泌和血糖的影响。给予ADPbetaS(0.2 mg kg-1)会产生依赖于动物营养状态的胰岛素反应，因为我们只观察到隔夜禁食大鼠的短暂增加，以及喂食大鼠持续的胰岛素分泌和血糖水平的下降。在静脉注射过程中。糖耐量试验，ADPbetaS促进胰岛素释放，从而增加葡萄糖消失率。给予ADPbetaS(0.1 mg·kg~(-1))可增加胰腺十二指肠胰岛素的排出量，并使血糖水平略有下降。4在清醒禁食犬中，口服ADPbetaS(0.1 mg·kg~(-1))可一过性升高胰岛素血症，并能及时降低血糖。此外，在口服葡萄糖耐量试验中，口服相同剂量的ADPbetaS显著促进胰岛素分泌，从而降低高血糖。5综上所述，P2y激动剂ADPbetaS在体内是一种有效的胰岛素促分泌剂，改善糖耐量，口服后有效。因此，β细胞的P2y-嘌呤受体可能是新药的靶点。
1 In vivo effect of a P2y-purinoceptor agonist, adenosine-5'-O-(2-thiodiphosphate) (ADPbetaS), on insulin secretion and glycaemia were studied both in rats and dogs.2 In anaesthetized rats, i.v. administered ADPbetaS (0.2 mg kg-1) produced an insulin response dependent on the nutritional state of the animals, since we observed only a transient increase in overnight-fasted rats and a sustained insulin secretion followed by a reduction in plasma glucose levels in fed rats. During an i.v. glucose tolerance test, ADPbetaS enhanced insulin release and thus increased the glucose disappearance rate.3 In anaesthetized fasted dogs, i.v. administered ADPbetaS (0.1 mg kg-1) increased pancreaticoduodenal insulin output and slightly decreased blood glucose levels.4 In conscious fasted dogs, orally administered ADPbetaS (0.1 mg kg-1) transiently increased insulinemia and punctually reduced glycaemia. Furthermore, during an oral glucose tolerance test, orally administered ADPbetaS at the same dose markedly enhanced insulin secretion and consequently reduced the hyperglycaemia.5 In conclusion, the P2y-agonist, ADPbetaS, is a potent insulin secretagogue in vivo, improves glucose tolerance and is effective after oral administration. Thus, the P2y-purinoceptors of the beta cell may be a target for new antidiabetic drugs.