T. Bridges

发表

Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model.

A. Levey, D. Brody, C. Lindsley, 2017, ACS chemical neuroscience.

Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.

C. Lindsley, C. Hopkins, M. Bubser, 2018, ACS chemical neuroscience.

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.

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.

J. Bartolomé-Nebreda, Sergio A Alonso de Diego, M. Martín-Martín, 2016, Bioorganic & medicinal chemistry letters.

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.

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

A. Megens, X. Langlois, J. Bartolomé-Nebreda, 2015, ACS 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.

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Brian A. Chauder, Bruce J. Melancon, D. Sheffler, 2012, Bioorganic & medicinal chemistry letters.

Discovery and development of a second highly selective M1 Positive Allosteric Modulator (PAM)

C. Lindsley, C. Weaver, E. Dawson, 2010 .

Discovery of the first mAChR 5 (M5) selective ligand, an M5 Positive Allosteric Modulator (PAM)

C. Lindsley, C. Weaver, L. M. Lewis, 2010 .

Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity

C. Lindsley, P. Conn, C. Niswender, 2010 .

Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

D. Sheffler, C. Lindsley, E. Lebois, 2012, ACS chemical neuroscience.

Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, D. Sheffler, 2013, 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.

Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.

C. Lindsley, R. Breyer, R. Morrison, 2013, Bioorganic & medicinal chemistry letters.

Design of potent GlyT1 inhibitors: in vitro and in vivo profiles.

C. Lindsley, R. Williams, T. Bridges, 2008, Current opinion in molecular therapeutics.

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

D. Sheffler, C. Lindsley, Hyekyung P. Cho, 2011, Bioorganic & medicinal chemistry letters.

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.

S. Jadhav, C. Lindsley, Joy E. Marlo, 2009, Journal of medicinal chemistry.

Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity

C. Lindsley, H. Brown, Joy E. Marlo, 2009, Molecular Pharmacology.

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

J. P. Kennedy, C. Lindsley, C. Hopkins, 2010, Bioorganic & medicinal chemistry letters.

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.

Microsoft Word-32670823-file00.docx

T. Daigle, C. Mackie, H. Lavreysen, 2013 .

Development and characterization of a highly selective M5 PAM probe molecule with improved potency

Julie L. Engers, C. Lindsley, P. Conn, 2013 .

Evaluation of intravitreal topotecan dose levels, toxicity and efficacy for retinoblastoma vitreous seeds: a preclinical and clinical study

C. Lindsley, D. Friedman, K. Boyd, 2021, British Journal of Ophthalmology.

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.

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.

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.

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.

The antipsychotic potential of muscarinic allosteric modulation.

C. Lindsley, C. Hopkins, E. Lebois, 2010, Drug news & perspectives.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 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.

Application of combinatorial chemistry science on modern drug discovery.

Craig W Lindsley, J. P. Kennedy, C. Lindsley, 2008, Journal of combinatorial chemistry.

Preparation of Unsymmetrical 1,2,4,5-Tetrazines via a Mild Suzuki Cross-Coupling Reaction.

C. Lindsley, Aaron M. Bender, T. Bridges, 2017, Organic letters.

Lead Optimization in Drug Discovery

Thomas M. Bridges, Craig W. Lindsley, David Weaver, 2008 .

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

K. Gregory, C. Lindsley, C. Hopkins, 2016, Chemical reviews.

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

Kari A. Johnson, K. Gregory, J. Bartolomé-Nebreda, 2015, Neuron.

A Selective Allosteric Potentiator of the M1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning

M. Quirk, A. Levey, E. Christian, 2009, The Journal of Neuroscience.

Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154

J. Wess, N. Brandon, C. Lindsley, 2018, Neuropharmacology.

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.

Phosphodiesterase 10 A Regulates Alcohol and Saccharin Self-Administration in Rats

Robert L Barry, John C Gore, P Jeffrey Conn, 2014 .

Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Julie L. Engers, C. Lindsley, P. Conn, 2013, Bioorganic & medicinal chemistry letters.

Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

D. Sheffler, C. Lindsley, P. Conn, 2012, Bioorganic & medicinal chemistry letters.

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

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

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.

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.

C. Lindsley, P. Conn, R. Daniels, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.

J. P. Kennedy, C. Lindsley, P. Conn, 2008, Bioorganic & medicinal chemistry letters.

Novel Selective Allosteric Activator of the M1 Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats

A. Deutch, A. Levey, R. Kessler, 2008, The Journal of Neuroscience.

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

D. Sheffler, J. P. Kennedy, C. Lindsley, 2008, Bioorganic & medicinal chemistry letters.

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2017, ACS medicinal chemistry letters.

A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning

S. Jadhav, D. Sheffler, Z. Xiang, 2009, Molecular Pharmacology.

N-Aryl Piperazine Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators Possess Efficacy in Preclinical Models of NMDA Hypofunction and Cognitive Enhancement

M. Caron, S. Jadhav, K. Gregory, 2013, The Journal of Pharmacology and Experimental Therapeutics.

The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with l-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease

Anna L. Blobaum, M. Amalric, S. Jadhav, 2012, Journal of Pharmacology and Experimental Therapeutics.

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 .

mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome.

C. Lindsley, P. Conn, S. Stauffer, 2016, Human molecular genetics.

Pharmacokinetics, Tissue Localization, Toxicity, and Treatment Efficacy in the First Small Animal (Rabbit) Model of Intra-Arterial Chemotherapy for Retinoblastoma

C. Lindsley, D. Friedman, K. Boyd, 2018, Investigative ophthalmology & visual science.

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, ACS chemical neuroscience.

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.

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

Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249.

C. Lindsley, Takahiro Mori, D. Engers, 2019, Bioorganic & medicinal chemistry letters.

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.

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.

Evaluation of 1,2,3-Triazoles as Amide Bioisosteres In Cystic Fibrosis Transmembrane Conductance Regulator Modulators VX-770 and VX-809.

Wei Wang, Liping Tang, S. Rowe, 2019, Chemistry.

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.

Julie L. Engers, C. Lindsley, P. Conn, 2021, ACS medicinal chemistry letters.

G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms.

C. Lindsley, T. Bridges, 2008, ACS chemical biology.

Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice

Z. Xiang, C. Lindsley, P. Conn, 2015, Proceedings of the National Academy of Sciences.

Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2021, ACS pharmacology & translational science.

Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats

S. Jadhav, J. P. Kennedy, C. Lindsley, 2008, Journal of Pharmacology and Experimental Therapeutics.

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.

Intravitreal HDAC Inhibitor Belinostat Effectively Eradicates Vitreous Seeds Without Retinal Toxicity In Vivo in a Rabbit Retinoblastoma Model

Yuankai K. Tao, C. Lindsley, D. Friedman, 2021, Investigative ophthalmology & visual science.

Catalytic site amino acids of PKGI-alpha influence allosteric cGMP binding.

J. Corbin, T. M. Bridges, S. Francis, 2013, Frontiers in bioscience.

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

S. Jadhav, J. Meiler, Z. Xiang, 2010, ACS chemical neuroscience.

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

S. Jadhav, J. Meiler, Z. Xiang, 2010, ACS chemical neuroscience.

Modulation of arousal and sleep/wake architecture by M1 PAM VU0453595 across young and aged rodents and nonhuman primates

Anna L. Blobaum, M. Nader, P. Newhouse, 2020, Neuropsychopharmacology.

Synthesis and Characterization of Chiral 6-Azaspiro[2.5]Octanes as Potent and Selective Antagonists of the M4 Muscarinic Acetylcholine Receptor

C. Lindsley, P. Conn, J. Harp, 2021, Bioorganic & Medicinal Chemistry Letters.

Acute Negative Allosteric Modulation of M5 Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with no effect on Antinociception.

C. Lindsley, D. Winder, R. Matthews, 2019, ACS chemical neuroscience.

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

D. Sheffler, Z. Xiang, C. Lindsley, 2011, Bioorganic & medicinal chemistry letters.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Peter Chase, P Jeffrey Conn, Craig W Lindsley, 2013, Journal of medicinal chemistry.

M5 Receptor Activation Produces Opposing Physiological Outcomes in Dopamine Neurons Depending on the Receptor's Location

D. Sulzer, Z. Xiang, C. Lindsley, 2014, The Journal of Neuroscience.

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.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Alice E. Berizzi, C. Langmead, P. Sexton, 2018, ACS chemical neuroscience.

Development of a Novel, Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype Selectivity

Julie L. Engers, C. Lindsley, P. Conn, 2015 .

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 of the first selective M4 muscarinic acetylcholine receptor antagonists with in vivo anti-parkinsonian and anti-dystonic efficacy

Julie L. Engers, C. Lindsley, P. Conn, 2020 .

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.

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies.

C. Lindsley, P. Conn, Kellie D. Nance, 2017, Bioorganic & medicinal chemistry letters.

Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.

Julie L. Engers, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes.

Julie L. Engers, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Alison R. Gregro, Andrew S. Felts, N. Schnetz-Boutaud, 2019, Bioorganic & medicinal chemistry letters.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

C. Lindsley, P. Conn, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.

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

Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Alison R. Gregro, Julie L. Engers, C. Lindsley, 2019, 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.

Synthesis and Structure–Activity Relationships of Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor

J. P. Kennedy, C. Lindsley, P. Conn, 2009, ChemMedChem.

Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.

C. Hopkins, C. Weaver, R. Morrison, 2017, ACS chemical neuroscience.

The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU 0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2 A Antagonist in Preclinical Rodent Models of Parkinson ’ s Disease

Anna L. Blobaum, M. Amalric, S. Jadhav, 2012 .

Discovery and development of the a highly selective M1 Positive Allosteric Modulator (PAM)

C. Lindsley, C. Weaver, E. Dawson, 2010 .

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, P. Conn, 2013, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & Medicinal Chemistry Letters.

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.

J. P. Kennedy, C. Lindsley, C. Hopkins, 2010, Bioorganic & medicinal chemistry letters.

Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.

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

J. Bartolomé-Nebreda, M. Martín-Martín, Carlos M Martínez-Viturro, 2016, Bioorganic & medicinal chemistry letters.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Alison R. Gregro, Julie L. Engers, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

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.

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

Stephen M. Damon, A. Deutch, J. Wess, 2014, Neuropsychopharmacology.

N-Aryl Piperazine Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators Possess Efficacy in Preclinical Models of NMDA Hypofunction and Cognitive Enhancement

S. Jadhav, H. Lavreysen, C. Lindsley, 2013, The Journal of Pharmacology and Experimental Therapeutics.

Title: N -aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in pre-clinical models of NMDA hypofunction and cognitive enhancement

T. Daigle, C. Mackie, H. Lavreysen, 2013 .

Scheme 1, Reagents and conditions

C. Lindsley, P. Conn, C. Weaver, 2013 .

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Alison R. Gregro, Andrew S. Felts, N. Brandon, 2019, Bioorganic & 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.

Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats

S. Jadhav, J. P. Kennedy, C. Lindsley, 2008, Journal of Pharmacology and Experimental Therapeutics.

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, Margrith E. Mattmann, 2013, Bioorganic & medicinal chemistry letters.

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

DMD052662 2066..2075

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

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

A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning

S. Jadhav, D. Sheffler, C. Lindsley, 2009, Molecular Pharmacology.