21314-80-7Relevant academic research and scientific papers
Imidazolines as efficacious glucose-dependent stimulators of insulin secretion
Jakobsen, Palle,Madsen, Peter,Andersen, HenrikSune
, p. 357 - 362 (2003)
Synthesis of a series of imidazolines with glucose dependent effects on insulin exocytosis from pancreatic β-cells is reported. Regioisomers and enantiomers were found to exhibit marked differences in exocytotic effects as well as different activities on the KATP-channel; the (R (+)) isomer of 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-thiophene-2-ylethyl]pyridin e (4a) and the (+) isomer of 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-thiophene-3-ylethyl]pyridin e (4d) were found to give a significant increase in insulin release - in contrast to findings for their enantiomers - without influence on the KATP-channel. The (+) isomer (4a) showed glucose dependent insulin release from β-cells at concentrations above 2.5 mM and a marked glucose lowering effect in ob/ob mice as well as in fed but not in fasted rats.
Oral hypoglycaemic agents
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, (2008/06/13)
Compounds of formula (I) which are optionally substituted 2-(ω,ω-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(ω,ω-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. T
