Variations in tissue selectivity amongst insulin secretagogues: a systematic review

被引：73

作者：

Abdelmoneim, A. S. ^{[1
]}

Hasenbank, S. E. ^{[1
]}

Seubert, J. M. ^{[1
,2
]}

Brocks, D. R. ^{[1
]}

Light, P. E. ^{[2
]}

Simpson, S. H. ^{[1
]}

机构：

[1] Univ Alberta, Fac Pharm & Pharmaceut Sci, Dent Pharm Ctr 3126, Edmonton, AB T6G 2N8, Canada

[2] Univ Alberta, Fac Med, Dept Pharmacol, Edmonton, AB T6G 2N8, Canada

来源：

DIABETES OBESITY & METABOLISM | 2012年 / 14卷 / 02期

基金：

加拿大健康研究院;

关键词：

insulin secretagogues; ischaemic preconditioning; sulfonylurea receptor; K-ATP CHANNELS; SENSITIVE POTASSIUM-CHANNELS; BETA-CELL; MYOCARDIAL-INFARCTION; DIABETIC-PATIENTS; SULFONYLUREA DRUGS; VASCULAR COMPLICATIONS; HYPOGLYCEMIC AGENTS; GLIMEPIRIDE BLOCK; HIGH-AFFINITY;

D O I：

10.1111/j.1463-1326.2011.01496.x

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Aim: Insulin secretagogues promote insulin release by binding to sulfonylurea receptors on pancreatic beta-cells (SUR1). However, these drugs also bind to receptor isoforms on cardiac myocytes (SUR2A) and vascular smooth muscle (SUR2B). Binding to SUR2A/SUR2B may inhibit ischaemic preconditioning, an endogenous protective mechanism enabling cardiac tissue to survive periods of ischaemia. This study was designed to identify insulin secretagogues that selectively bind to SUR1 when given at therapeutic doses.

引用

页码：130 / 138

页数：9

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