Lenti G, Pagano G, Angotzi G, Sani A B, Diana A
Eur J Clin Pharmacol. 1975 Dec 19;9(2-3):189-92. doi: 10.1007/BF00614016.
A xanthine derivative, named BL-191, was administered iv in 8 healthy volunteers alone and in association with glucose (0.33 g/kg body weight iv) or glybenclamide (1 mg iv). BL-191 was infused iv at a constant rate in a dose of 200 mg during 45 minutes. Blood glucose, free fatty acids and immunoreactive insulin were measured during one hour. It was impossible to demonstrate neither a direct effect nor an enhancement of insulin secretion during drug administration; in another experiment (treatment F) a higher dosage of BL-191 (100 mg as a priming dose + 200 mg as infusion dose) was likely ineffective. It appears that some difference in insulin response may be present in the single subject (not evident in the mean), indicating a difference in the beta-cell cAMP-system sensitivity in individuals. These negative results allow some considerations on the importance of the beta-cell cAMP-system in healthy human beings.
一种名为BL - 191的黄嘌呤衍生物,单独以及与葡萄糖(静脉注射0.33 g/kg体重)或格列本脲(静脉注射1 mg)联合,静脉注射给8名健康志愿者。在45分钟内以200 mg的剂量恒速静脉输注BL - 191。在一小时内测量血糖、游离脂肪酸和免疫反应性胰岛素。在给药期间,既无法证明其对胰岛素分泌有直接作用,也无法证明其增强胰岛素分泌;在另一项实验(治疗F)中,更高剂量的BL - 191(100 mg作为起始剂量 + 200 mg作为输注剂量)可能无效。似乎在单个受试者中可能存在胰岛素反应的某些差异(在平均值中不明显),表明个体中β细胞环磷酸腺苷(cAMP)系统敏感性存在差异。这些阴性结果引发了对β细胞cAMP系统在健康人类中的重要性的一些思考。