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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 May 07; Vol. 3 (6), pp. 484-9. Date of Electronic Publication: 2012 May 07 (Print Publication: 2012). - Publication Year :
- 2012
-
Abstract
- A structure-activity relationship study of the imidazolyl-β-tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which demonstrated superior efficacy in a mouse oGTT model. MK-4256 reduced glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po. As compared with glipizide, MK-4256 showed a minimal hypoglycemia risk in mice.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 3
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900499
- Full Text :
- https://doi.org/10.1021/ml300063m