Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. Introducing a new discovery about 50675-18-8, Name is Tetrahydropyran-4-carbaldehyde, HPLC of Formula: C6H10O2.
This letter provides the first pharmacological proof of principle that the sst3 receptor mediates glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells. To enable these studies, we identified the selective sst3 antagonist (1R,3R)-3-(5-phenyl-1H-imidazol-2-yl)-1- (tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-beta-carboline (5a), with improved ion channel selectivity and mouse pharmacokinetic properties as compared to previously described tetrahydro-beta-carboline imidazole sst3 antagonists. We demonstrated that compound 5a enhances GSIS in pancreatic beta-cells and blocks glucose excursion induced by dextrose challenge in ipGTT and OGTT models in mice. Finally, we provided strong evidence that these effects are mechanism-based in an ipGTT study, showing reduction of glucose excursion in wild-type but not sst3 knockout mice. Thus, we have shown that antagonism of sst3 represents a new mechanism with potential in treating type 2 diabetes mellitus.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics