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GPR109a agonists. Part 2: Pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a
Authors:Jason E. Imbriglio  Sookhee Chang  Rui Liang  Subharekha Raghavan  Darby Schmidt  Abby Smenton  Scott Tria  Thomas O. Schrader  Jae-Kyu Jung  Craig Esser  Tom G. Holt  Michael S. Wolff  Andrew K.P. Taggart  Kang Cheng  Ester Carballo-Jane  M. Gerard Waters  James R. Tata  Steven L. Colletti
Affiliation:1. Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, United States;2. Department of Drug Metabolism, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, United States;3. Department of Cardiovascular Diseases, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, United States;4. Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, United States
Abstract:5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.
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