John T. Lazzaro

Pfizer (United States) — United States

Neuroscience · Life Sciences

17h-index912citations28works14.02yr avg
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Research Topics

Neuroscience and Neuropharmacology Research(17), Receptor Mechanisms and Signaling(10), Pharmacological Receptor Mechanisms and Effects(8), Chemical Synthesis and Analysis(4), Nicotinic Acetylcholine Receptors Study(4)

Publications28 total

Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M<sub>4</sub> Muscarinic Acetylcholine Receptor
Journal of Medicinal Chemistry·2024· 14 citedOpen Access
A role for the M1 muscarinic receptor in gastrointestinal motility
Journal of Pharmacological and Toxicological Methods·2019
Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline
ACS Chemical Neuroscience·2019· 9 cited
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres
ACS Medicinal Chemistry Letters·2019· 14 citedOpen Access
Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline
ACS Chemical Neuroscience·2018· 32 cited
Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program
Bioorganic & Medicinal Chemistry Letters·2018· 12 citedOpen Access
The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging
Journal of Medicinal Chemistry·2017· 36 cited
Discovery and Characterization of (<i>R</i>)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-<i>c</i>][1,4]oxazin-4(9<i>H</i>)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates
Journal of Medicinal Chemistry·2017· 9 citedOpen Access
Design and Synthesis of γ- and δ-Lactam M<sub>1</sub> Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M<sub>1</sub>-Selective PAM with Weak Agonist Activity
Journal of Medicinal Chemistry·2017· 58 citedOpen Access
Characterization of a Novel M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator Radioligand, [3H]PT-1284
Molecular Pharmacology·2016· 7 cited
Discovery of the Potent and Selective M1 PAM-Agonist<i>N</i>-[(3<i>R</i>,4<i>S</i>)-3-Hydroxytetrahydro-2<i>H</i>-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects
Journal of Medicinal Chemistry·2016· 83 citedOpen Access
Design and optimization of selective azaindole amide M1 positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters·2015· 44 citedOpen Access
The Discovery and Characterization of the α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Potentiator <i>N</i> -{(3 <i>S</i> ,4 <i>S</i> )-4-[4-(5-Cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)
Journal of Medicinal Chemistry·2015· 29 cited
CCDC 1402068: Experimental Crystal Structure Determination
The Cambridge Structural Database·2015Open Access
Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1 <i>H</i> -pyrazolo-[3,4- <i>b</i> ]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator
Journal of Medicinal Chemistry·2014· 51 citedOpen Access
Discovery and Characterization of a Novel Dihydroisoxazole Class of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) Receptor Potentiators
Journal of Medicinal Chemistry·2013· 22 cited
Positive Allosteric Modulation of AMPA Receptors from Efficacy to Toxicity: The Interspecies Exposure-Response Continuum of the Novel Potentiator PF-4778574
Journal of Pharmacology and Experimental Therapeutics·2013· 61 cited
1-[(1-Methyl-1<i>H</i>-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis
Journal of Medicinal Chemistry·2011· 31 citedOpen Access
Design, synthesis, structure-activity relationships, and biological evaluation of AMPA positive allosteric modulators (PAMs)
Abstracts of papers - American Chemical Society·2010
High-throughput Screening in Embryonic Stem Cell-derived Neurons Identifies Potentiators of α-Amino-3-hydroxyl-5-methyl-4-isoxazolepropionate-type Glutamate Receptors
Journal of Biological Chemistry·2010· 67 citedOpen Access
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Frequent Co-authors

Lei Zhang(10), Jeremy R. Edgerton(7), Susan M. Lotarski(7), Sarah Grimwood(7), Christopher L. Shaffer(7), Frank S. Menniti(6), Michael A. Brodney(6), Michael Popiolek(6), Stefanus J. Steyn(6), Raymond S Hurst(6), Alan H. Ganong(5), Jennifer E. Davoren(5), Jacob B. Schwarz(5), Dianne K. Bryce(5), Laigao Chen(5), Kenneth Zasadny(5), Frank E. Ewing(4), Che‐Wah Lee(4), Steven V. O’Neil(4), Damien Webb(4)