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MK-4256

 
National Institutes of Health

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Carbolines

Papers overview

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2016
2016
SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.
MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs… Expand
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2015
2015
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.
We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H… Expand
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2014
2014
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the… Expand
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2012
2012
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
A structure-activity relationship study of the imidazolyl-β-tetrahydrocarboline series identified MK-4256 as a potent, selective… Expand
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