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Sp-5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole-3',5'-cyclic monophosphorothioate is a potent stimulus for insulin release.

作者信息

Laychock S G

机构信息

Department of Pharmacology and Therapeutics, School of Medicine and Biomedical Sciences, State University of New York at Buffalo 14214.

出版信息

Endocr Res. 1993;19(2-3):113-22. doi: 10.3109/07435809309033018.

DOI:10.3109/07435809309033018
PMID:8287829
Abstract

The Sp-isomer of 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole-3',5'-cyclic monophosphorothioate (Sp-5,6-DCl-cBIMPS) at micromolar concentrations was a more potent stimulus for insulin release than 8-bromo-cyclic (c) AMP in isolated pancreatic islets of the rat. Sp-5,6-DCl-cBIMPS increased basal secretion, and potentiated glucose-stimulated insulin release to levels similar to those evoked by glucagon. A ten-fold higher concentration of 8-bromo-cAMP was required to mimic the potentiating effects of Sp-5,6-DCl-cBIMPS. Neither 8-para-chlorophenylthio-cGMP, 8-bromo-cGMP, nor dibutyryl-cGMP affected insulin release. Thus, Sp-5,6-DCl-cBIMPS is a potent and specific stimulus for cAMP-mediated insulin release.

摘要

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