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Synthesis and pharmacological characterization of C4-disubstituted analogs of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: identification of a potent, selective metabotropic glutamate receptor agonist and determination of agonist-bound human mGlu2 and mGlu3 amino terminal domain structures.
Monn JA, Prieto L, Taboada L, Pedregal C, Hao J, Reinhard MR, Henry SS, Goldsmith PJ, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Xiang C, Catlow JT, Swanson S, Sanger H, Broad LM, Johnson MP, Knopp KL, Simmons RM, Johnson BG, Shaw DB, McKinzie DL. Monn JA, et al. J Med Chem. 2015 Feb 26;58(4):1776-94. doi: 10.1021/jm501612y. Epub 2015 Feb 5. J Med Chem. 2015. PMID: 25602126
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist.
Monn JA, Prieto L, Taboada L, Hao J, Reinhard MR, Henry SS, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Getman BG, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL. Monn JA, et al. J Med Chem. 2015 Sep 24;58(18):7526-48. doi: 10.1021/acs.jmedchem.5b01124. J Med Chem. 2015. PMID: 26313429
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.
Liu B, Croy CH, Hitchcock SA, Allen JR, Rao Z, Evans D, Bures MG, McKinzie DL, Watt ML, Stuart Gregory G, Hansen MM, Hoogestraat PJ, Jamison JA, Okha-Mokube FM, Stratford RE, Turner W, Bymaster F, Felder CC. Liu B, et al. Among authors: bures mg. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4158-63. doi: 10.1016/j.bmcl.2015.08.011. Epub 2015 Aug 8. Bioorg Med Chem Lett. 2015. PMID: 26299349
23 results