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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2012 ; 3 (6): 484-9 Nephropedia Template TP
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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes #MMPMID24900499
He S; Ye Z; Truong Q; Shah S; Du W; Guo L; Dobbelaar P; Lai Z; Liu J; Jian T; Qi H; Bakshi RK; Hong Q; Dellureficio J; Pasternak A; Feng Z; deJesus R; Yang L; Reibarkh M; Bradley S; Holmes MA; Ball RG; Ruck RT; Huffman M; Wong F; Samuel K; Reddy VB; Mitelman S; Tong S; Chicchi GG; Tsao KL; Trusca D; Wu M; Shao Q; Trujillo M; Eiermann GJ; Li C; Zhang BB; Howard A; Zhou YP; Nargund RP; Hagmann WK
ACS Med Chem Lett 2012[Jun]; 3 (6): 484-9 PMID24900499show ga
A structure?activity relationship study of the imidazolyl-?-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.