M. Noetzel

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Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS

Kari A. Johnson, K. Gregory, P. Conn, 2014, The Journal of Neuroscience.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, N. Brandon, 2017, ACS medicinal chemistry letters.

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.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

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

Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

Andrew S. Felts, Brian A. Chauder, K. Gregory, 2012, Molecular Pharmacology.

Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

F. Dudek, K. Gregory, Z. Xiang, 2013, Biological Psychiatry.

A Novel Metabotropic Glutamate Receptor 5 Positive Allosteric Modulator Acts at a Unique Site and Confers Stimulus Bias to mGlu5 Signaling

K. Gregory, C. Lindsley, P. Conn, 2013, Molecular Pharmacology.

In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug Discovery.

K. Gregory, C. Lindsley, P. Conn, 2019, ACS pharmacology & translational science.

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.

J. Bartolomé-Nebreda, Carlos M Martínez-Viturro, G. Macdonald, 2015, Bioorganic & medicinal chemistry letters.

Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizure-Like Adverse Events in Rats Involving a Receptor Agonism-Dependent Mechanism

Z. Xiang, C. Lindsley, P. Conn, 2013, Drug Metabolism and Disposition.

Mechanisms of M3 Muscarinic Receptor Regulation by Wash-Resistant Xanomeline Binding

M. Noetzel, E. El-Fakahany, M. Grant, 2009, Pharmacology.

Functional impact of allosteric agonist activity of selective positive allosteric modulators of mGlu 5 in regulating CNS function

H. Lavreysen, Z. Xiang, C. Lindsley, 2011 .

Immediate and Delayed Consequences of Xanomeline Wash-Resistant Binding at the M3 Muscarinic Receptor

M. Noetzel, E. El-Fakahany, M. Grant, 2009, Neurochemical Research.

Radical reactions from missing ceruloplasmin

M. Noetzel, M. Noetzel, W. Graf, 1999, Neurology.

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.

C. Lindsley, P. Conn, P. R. Gentry, 2010, Bioorganic & medicinal chemistry letters.

Tetrahydronaphthyridine and Dihydronaphthyridinone Ethers As Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 5 (mGlu5)

S. Jadhav, J. Bartolomé-Nebreda, M. Martín-Martín, 2014, 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.

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

N. Brandon, C. Lindsley, P. Conn, 2016, Bioorganic & medicinal chemistry letters.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Alison R. Gregro, Julie L. Engers, Bruce J. Melancon, 2016, Bioorganic & medicinal chemistry letters.

Heparan sulfate mediates neuroprotection from degeneration in experimental glutaric aciduria

W. Low, M. Noetzel, Z. Demorest, 2006, Experimental Neurology.

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

J. Bartolomé-Nebreda, M. Martín-Martín, Carlos M Martínez-Viturro, 2015, Bioorganic & medicinal chemistry letters.

Synthesis and bioactivity of (±)-tetrahydrohaliclonacyclamine A

Brian J. Smith, C. Lindsley, T. Qu, 2010 .

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

K. Gregory, J. Meiler, Z. Xiang, 2013, Journal of medicinal chemistry.

Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders.

K. Gregory, C. Niswender, M. Noetzel, 2013, Progress in molecular biology and translational science.

Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

H. Lavreysen, Z. Xiang, C. Lindsley, 2012, Molecular Pharmacology.

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 – Relation to antipsychotic-like drug effects

N. Brandon, C. Lindsley, M. Ivarsson, 2016, Neuropharmacology.

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.

Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Emerging approaches for treatment of schizophrenia: modulation of glutamatergic signaling.

P. Conn, M. Noetzel, C. Jones, 2012, Discovery medicine.

Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models

M. Foster Olive, J. Scott Daniels, P. Jeffrey Conn, 2012, The Journal of Neuroscience.

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.

Peter Hodder, P. Jeffrey Conn, Craig W. Lindsley, 2015, Bioorganic & medicinal chemistry letters.

The action of xanomeline on human muscarinic receptors expressed in Chinese hamster ovary cells

M. Noetzel, 2009 .

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

Peter Hodder, Louis Scampavia, Franck Madoux, 2015, Journal of biomolecular screening.

Long-Term Changes in the Muscarinic M1 Receptor Induced by Instantaneous Formation of Wash-Resistant Xanomeline-Receptor Complex

Kayla C. De Lorme, M. Noetzel, E. El-Fakahany, 2007, Journal of Pharmacology and Experimental Therapeutics.

Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model

C. Lindsley, P. Conn, C. Niswender, 2016, Neuropsychopharmacology.

Preview : Published ahead of advance online publication

C. Lindsley, P. Conn, C. Niswender, 2015 .

Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.

Jens Meiler, P Jeffrey Conn, Jeffrey L. Mendenhall, 2014, ACS chemical neuroscience.

Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, Journal of medicinal chemistry.

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.

J. Bartolomé-Nebreda, H. Tong, G. Macdonald, 2014, Bioorganic & medicinal chemistry letters.

Allosteric Modulators of Metabotropic Glutamate Receptor 5 for Treatment of Schizophrenia

S. Jadhav, C. Lindsley, P. Conn, 2011 .

Epileptiform Discharges in Hippocampal Slices Role of Synaptic Metabotropic Glutamate Receptors in

R. Wong, Z. Xiang, P. Conn, 2015 .

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

S. Jadhav, J. Bartolomé-Nebreda, F. Delgado, 2013, Journal of medicinal chemistry.

Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

H. Lavreysen, C. Lindsley, Hyekyung P. Cho, 2012, Molecular Pharmacology.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

N. Brandon, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

C. Lindsley, P. Conn, C. Niswender, 2013 .