Sp-5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole-3',5'-cyclic monophosphorothioate is a potent stimulus for insulin release.
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.
Laychock
S G
SG
Department of Pharmacology and Therapeutics, School of Medicine and Biomedical Sciences, State University of New York at Buffalo 14214.
D015124:8-Bromo Cyclic Adenosine Monophosphate / Q000494:pharmacology; D000818:Animals; D006152:Cyclic GMP / Q000031:analogs & derivatives / Q000494:pharmacology; D004004:Dichlororibofuranosylbenzimidazole / Q000031:analogs & derivatives*; D007328:Insulin / Q000378:metabolism*; D000078790:Insulin Secretion; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013873:Thionucleotides / Q000494:pharmacology*
D007328:Insulin; D013873:Thionucleotides; C071644:5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole-3',5'-monophosphorothioate; D015124:8-Bromo Cyclic Adenosine Monophosphate; D004004:Dichlororibofuranosylbenzimidazole; C055656:8-((4-chlorophenyl)thio)cyclic-3',5'-GMP; D006152:Cyclic GMP