Frank W. Byers

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Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

N. Brandon, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2016, Bioorganic & medicinal chemistry letters.

Use of a novel rapid and resource-efficient cassette dosing approach to determine the pharmacokinetics and CNS distribution of small molecule 7-transmembrane receptor allosteric modulators in rat

T. M. Bridges, R. Morrison, Frank W. Byers, 2014, Pharmacology research & perspectives.

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2013, Bioorganic & medicinal chemistry letters.

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2018, Bioorganic & medicinal chemistry letters.

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2015, Bioorganic & medicinal chemistry letters.

Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)‐Selective M5‐Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, ChemMedChem.

Emerging Novel Enzyme Pathways in Drug Metabolism Evaluating the Disposition of a Mixed Aldehyde Oxidase / Cytochrome P 450 Substrate in Rats with Attenuated P 450 Activity s

C. Lindsley, R. Morrison, Frank W. Byers, 2016 .

Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

Andrew S. Felts, C. Lindsley, P. Conn, 2016, Neuropsychopharmacology.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics

Anna L. Blobaum, Z. Xiang, C. Lindsley, 2015, Journal of medicinal chemistry.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Bruce J. Melancon, Z. Xiang, O. McManus, 2011, ACS chemical neuroscience.

Evaluating the Disposition of a Mixed Aldehyde Oxidase/Cytochrome P450 Substrate in Rats with Attenuated P450 Activity

C. Lindsley, R. Morrison, Frank W. Byers, 2016, Drug Metabolism and Disposition.

Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

Bruce J. Melancon, J. Wess, N. Brandon, 2014, ACS chemical neuroscience.

Heterotropic Activation of the Midazolam Hydroxylase Activity of CYP3A by a Positive Allosteric Modulator of mGlu5: In Vitro to In Vivo Translation and Potential Impact on Clinically Relevant Drug-Drug Interactions

Anna L. Blobaum, G. Macdonald, H. Lavreysen, 2013, Drug Metabolism and Disposition.

Microsoft Word-JSD_3A4_activation_mGlu5_PAM_revised_final_V4[1]

Anna L. Blobaum, G. Macdonald, H. Lavreysen, 2013 .

DMD052662 2066..2075

Anna L. Blobaum, G. Macdonald, H. Lavreysen, 2013 .

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo

Anna L. Blobaum, C. Lindsley, P. Conn, 2015, Drug Metabolism and Disposition.

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2015, Journal of medicinal chemistry.

Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.

Andrew S. Felts, C. Lindsley, P. Conn, 2013, ACS chemical neuroscience.

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

Julie L. Engers, Andrew S. Felts, Anna L. Blobaum, 2015, Journal of medicinal chemistry.

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Andrew S. Felts, C. Lindsley, Hyekyung P. Cho, 2013, Bioorganic & medicinal chemistry letters.

The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2012, Drug Metabolism and Disposition.

The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of mGlu5

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2012 .

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2017, Journal of medicinal chemistry.

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).

Julie L. Engers, Andrew S. Felts, C. Lindsley, 2013, Journal of medicinal chemistry.

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).

Julie L. Engers, Andrew S. Felts, Cody J. Wenthur, 2013, Journal of medicinal chemistry.

H. Lavreysen, C. Lindsley, Margrith E. Mattmann, 2013, Drug Metabolism and Disposition.

DMD052662 2066..2075

H. Lavreysen, C. Lindsley, Margrith E. Mattmann, 2013 .