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一种黄嘌呤衍生物(BL 191)对正常男性胰岛素分泌的影响。

Effects of a xanthine derivative (BL 191) on insulin secretion in normal man.

作者信息

Lenti G, Pagano G, Angotzi G, Sani A B, Diana A

出版信息

Eur J Clin Pharmacol. 1975 Dec 19;9(2-3):189-92. doi: 10.1007/BF00614016.

DOI:10.1007/BF00614016
PMID:823033
Abstract

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.

摘要

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。

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引用本文的文献

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本文引用的文献

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Adenosine 3',5'-phosphate in biological materials. I. Purification and properties of cyclic 3',5'-nucleotide phosphodiesterase and use of this enzyme to characterize adenosine 3',5'-phosphate in human urine.生物材料中的3',5'-磷酸腺苷。I. 环3',5'-核苷酸磷酸二酯酶的纯化及性质,以及用该酶鉴定人尿中的3',5'-磷酸腺苷
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Stimulation of insulin secretion by theophylline.茶碱对胰岛素分泌的刺激作用。
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己酮可可碱。对其药效学和药代动力学特性以及治疗效果的综述。
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The role of adenosine 3':5'-cyclic monophosphate in the regulation of insulin release by isolated rat islets of Langerhans.3':5'-环磷酸腺苷在离体大鼠胰岛调节胰岛素释放中的作用
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Perifusion of rat pancreatic tissue in vitro: substrate modification of theophylline-induced biphasic insulin release.大鼠胰腺组织的体外灌流:茶碱诱导的双相胰岛素释放的底物修饰
J Clin Invest. 1970 Nov;49(11):2097-105. doi: 10.1172/JCI106427.
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The role of cyclic AMP in the control of carbohydrate metabolism.环磷酸腺苷在碳水化合物代谢调控中的作用。
Diabetes. 1969 Dec;18(12):797-819. doi: 10.2337/diab.18.12.797.
9
A possible role for the adenylcyclase system in insulin secretion.腺苷酸环化酶系统在胰岛素分泌中的可能作用。
J Clin Invest. 1967 Nov;46(11):1724-34. doi: 10.1172/JCI105663.
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Progress in oral therapy of diabetes mellitus with sulphonylureas of the second generation.
Acta Diabetol Lat. 1972 Nov-Dec;9(6):865-99. doi: 10.1007/BF01564590.