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Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: wright ra. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis.
Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, Reinhard MR, Cohen MP, Hellman SL, Getman BG, Wang X, Menezes MM, Maren DL, Falcone JF, Anderson WH, Wright RA, Morin SM, Knopp KL, Adams BL, Rogovoy B, Okun I, Suter TM, Statnick MA, Gehlert DR, Nelson DL, Lucaites VL, Emkey R, DeLapp NW, Wiernicki TR, Cramer JW, Yang CR, Bruns RF. Svensson KA, et al. Among authors: wright ra. J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. doi: 10.1124/jpet.116.236372. Epub 2016 Nov 3. J Pharmacol Exp Ther. 2017. PMID: 27811173 Free PMC article.
Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
Dominguez C, Prieto L, Valli MJ, Massey SM, Bures M, Wright RA, Johnson BG, Andis SL, Kingston A, Schoepp DD, Monn JA. Dominguez C, et al. Among authors: wright ra. J Med Chem. 2005 May 19;48(10):3605-12. doi: 10.1021/jm040222y. J Med Chem. 2005. PMID: 15887967
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
Monn JA, Massey SM, Valli MJ, Henry SS, Stephenson GA, Bures M, Hérin M, Catlow J, Giera D, Wright RA, Johnson BG, Andis SL, Kingston A, Schoepp DD. Monn JA, et al. Among authors: wright ra. J Med Chem. 2007 Jan 25;50(2):233-40. doi: 10.1021/jm060917u. J Med Chem. 2007. PMID: 17228865
Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties.
Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Monn JA, et al. Among authors: wright ra. J Med Chem. 1997 Feb 14;40(4):528-37. doi: 10.1021/jm9606756. J Med Chem. 1997. PMID: 9046344
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors.
Monn JA, Valli MJ, Massey SM, Hansen MM, Kress TJ, Wepsiec JP, Harkness AR, Grutsch JL Jr, Wright RA, Johnson BG, Andis SL, Kingston A, Tomlinson R, Lewis R, Griffey KR, Tizzano JP, Schoepp DD. Monn JA, et al. Among authors: wright ra. J Med Chem. 1999 Mar 25;42(6):1027-40. doi: 10.1021/jm980616n. J Med Chem. 1999. PMID: 10090786
Structural Determinants of the γ-8 TARP Dependent AMPA Receptor Antagonist.
Lee MR, Gardinier KM, Gernert DL, Schober DA, Wright RA, Wang H, Qian Y, Witkin JM, Nisenbaum ES, Kato AS. Lee MR, et al. Among authors: wright ra. ACS Chem Neurosci. 2017 Dec 20;8(12):2631-2647. doi: 10.1021/acschemneuro.7b00186. Epub 2017 Sep 5. ACS Chem Neurosci. 2017. PMID: 28825787
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
Collado I, Pedregal C, Bueno AB, Marcos A, González R, Blanco-Urgoiti J, Pérez-Castells J, Schoepp DD, Wright RA, Johnson BG, Kingston AE, Moher ED, Hoard DW, Griffey KI, Tizzano JP. Collado I, et al. Among authors: wright ra. J Med Chem. 2004 Jan 15;47(2):456-66. doi: 10.1021/jm030967o. J Med Chem. 2004. PMID: 14711315
C3'-cis-Substituted carboxycyclopropyl glycines as metabotropic glutamate 2/3 receptor agonists: synthesis and SAR studies.
González R, Collado I, de Uralde BL, Marcos A, Martín-Cabrejas LM, Pedregal C, Blanco-Urgoiti J, Pérez-Castells J, Fernández MA, Andis SL, Johnson BG, Wright RA, Schoepp DD, Monn JA. González R, et al. Among authors: wright ra. Bioorg Med Chem. 2005 Dec 1;13(23):6556-70. doi: 10.1016/j.bmc.2005.07.036. Epub 2005 Sep 8. Bioorg Med Chem. 2005. PMID: 16153851
In Vitro Pharmacological Characterization and In Vivo Validation of LSN3172176 a Novel M1 Selective Muscarinic Receptor Agonist Tracer Molecule for Positron Emission Tomography.
Mogg AJ, Eessalu T, Johnson M, Wright R, Sanger HE, Xiao H, Crabtree MG, Smith A, Colvin EM, Schober D, Gehlert D, Jesudason C, Goldsmith PJ, Johnson MP, Felder CC, Barth VN, Broad LM. Mogg AJ, et al. J Pharmacol Exp Ther. 2018 Jun;365(3):602-613. doi: 10.1124/jpet.117.246454. Epub 2018 Apr 11. J Pharmacol Exp Ther. 2018. PMID: 29643252 Free PMC article.
291 results