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Review ArticleReview

Pharmacological Agents That Directly Modulate Insulin Secretion

Máire E. Doyle and Josephine M. Egan
Pharmacological Reviews March 2003, 55 (1) 105-131; DOI: https://doi.org/10.1124/pr.55.1.7
Máire E. Doyle
Diabetes Section, National Institute on Aging, National Institutes of Health, Baltimore, Maryland
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Josephine M. Egan
Diabetes Section, National Institute on Aging, National Institutes of Health, Baltimore, Maryland
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Abstract

Blood glucose levels are sensed and controlled by the release of hormones from the islets of Langerhans in the pancreas. The β-cell, the insulin-secreting cell in the islet, can detect subtle increases in circulating glucose levels and a cascade of molecular events spanning the initial depolarization of the β-cell membrane culminates in exocytosis and optimal insulin secretion. Here we review these processes in the context of pharmacological agents that have been shown to directly interact with any stage of insulin secretion. Drugs that modulate insulin secretion do so by opening the KATPchannels, by interacting with cell-surface receptors, by altering second-messenger responses, by disrupting the β-cell cytoskeletal framework, by influencing the molecular reactions at the stages of transcription and translation of insulin, and/or by perturbing exocytosis of the insulin secretory vesicles. Drugs acting primarily at the KATP channels are the sulfonylureas, the benzoic acid derivatives, the imidazolines, and the quinolines, which are channel openers, and finally diazoxide, which closes these channels. Methylxanthines also work at the cell membrane level by antagonizing the purinergic receptors and thus increase insulin secretion. Other drugs have effects at multiple levels, such as the calcineurin inhibitors and somatostatin. Some drugs used extensively in research, e.g., colchicine, which is used to study vesicular transport, have no effect at the pharmacological doses used in clinical practice. We also briefly discuss those drugs that have been shown to disrupt β-cell function in a clinical setting but for which there is scant information on their mechanism of action.

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Pharmacological Reviews: 55 (1)
Pharmacological Reviews
Vol. 55, Issue 1
1 Mar 2003
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Review ArticleReview

Pharmacological Agents That Directly Modulate Insulin Secretion

Máire E. Doyle and Josephine M. Egan
Pharmacological Reviews March 1, 2003, 55 (1) 105-131; DOI: https://doi.org/10.1124/pr.55.1.7

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Review ArticleReview

Pharmacological Agents That Directly Modulate Insulin Secretion

Máire E. Doyle and Josephine M. Egan
Pharmacological Reviews March 1, 2003, 55 (1) 105-131; DOI: https://doi.org/10.1124/pr.55.1.7
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  • Article
    • Abstract
    • I. Introduction
    • II. Insulin Synthesis and Secretion
    • III. Pharmaceutical Agents Active in the Treatment of Disorders of Glucose Homeostasis
    • IV. Drugs Administered in the Treatment of Disorders Other Than Diabetes That Have Effects on Pancreatic Insulin Secretion and β-Cell Function
    • Acknowledgments
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