S. Grimwood

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S Grimwood, S. Grimwood, Sarah Grimwood,, Sarah Grimwood
Publication record
90 papers · 2,847 citations · H-index 34

PAPERS

Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
202411 citationsauthor #15
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.
201911 citationsauthor #6
Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors.
201719 citationsauthor #13
Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.
201749 citationsauthor #7
Design and optimization of selective azaindole amide M1 positive allosteric modulators.
201640 citationsauthor #10
Erratum to: Translational Modeling in Schizophrenia: Predicting Human Dopamine D2 Receptor Occupancy
20161 citationsauthor #6
Translational Modeling in Schizophrenia: Predicting Human Dopamine D2 Receptor Occupancy
201618 citationsauthor #6
Characterization of a Novel M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator Radioligand, [3H]PT-1284
20167 citationsauthor #8
Erratum to: Translational Modeling in Schizophrenia: Predicting Human Dopamine D2 Receptor Occupancy
20160 citationsauthor #6
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-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.
201675 citationsauthor #27
Characterization of [11C]Lu AE92686 as a PET radioligand for phosphodiesterase 10A in the nonhuman primate brain
20168 citationsauthor #9
Inositol Phosphate Accumulation in Vivo Provides a Measure of Muscarinic M1 Receptor Activation.
201613 citationsauthor #9
Amphetamine Decreases α2C-Adrenoceptor Binding of [11C]ORM-13070: A PET Study in the Primate Brain
201519 citationsauthor #14
Application of cross-species PET imaging to assess neurotransmitter release in brain
20152 citationsauthor #11
Translational Modeling in Schizophrenia: Predicting Human Dopamine D2 Receptor Occupancy
20150 citationsauthor #6
Application of cross-species PET imaging to assess neurotransmitter release in brain
201568 citationsauthor #11
Dopamine D2 Receptor Occupancy as a Predictor of Catalepsy in Rats: A Pharmacokinetic-Pharmacodynamic Modeling Approach
201411 citationsauthor #6
Design, synthesis and evaluation of [(3)H]PF-7191, a highly specific nociceptin opioid peptide (NOP) receptor radiotracer for in vivo receptor occupancy (RO) studies.
201414 citationsauthor #6
Poster #S45 DEVELOPMENT OF NOVEL PET LIGANDS (PF-04831704 AND PF-06327104) FOR PDE10A
20141 citationsauthor #7
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
201451 citationsauthor #14
Evaluation of the agonist PET radioligand [11C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test-retest reproducibility and receptor occupancy by the antagonist PF-04455242
201452 citationsauthor #10
Highly Potent , Selective , and E ffi cacious Metabotropic Glutamate Receptor 5 ( mGluR 5 ) Negative Allosteric Modulator
20140 citationsauthor #16
Electrophysiological recordings in rats performing the sustained attention task
20130 citationsauthor #5
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.
2013172 citationsauthor #7
[11C]RO6899880, a novel agonist PET radioligand for the GABAA receptor
20132 citationsauthor #7
Neurophysiological signals as potential translatable biomarkers for modulation of metabotropic glutamate 5 receptors.
201318 citationsauthor #5
An investigation of metabotropic glutamate receptor 5 negative allosteric modulators in physiological and behavioral indicators of anxiety and cognition in rodents
20130 citationsauthor #6
Pharmacokinetic-pharmacodynamic modeling of the relationship between D2 receptor occupancy and catalepsy in rats
20120 citationsauthor #6
P2‐074: Modulation of soluble APPα in brain by PF‐04995274, a 5HT4 partial agonist, following single oral doses in healthy human volunteers: Study design and PK‐PD analysis
20121 citationsauthor #7
Pharmacokinetic-Pharmacodynamic Modeling of the D2 and 5-HT2A Receptor Occupancy of Risperidone and Paliperidone in Rats
201237 citationsauthor #6
The 5-Hydroxytryptamine4 Receptor Agonists Prucalopride and PRX-03140 Increase Acetylcholine and Histamine Levels in the Rat Prefrontal Cortex and the Power of Stimulated Hippocampal θ Oscillations
201254 citationsauthor #3
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
201244 citationsauthor #18
Pharmacokinetic-pharmacodynamic modeling of the relationship between D2 receptor occupancy and catalepsy in rats: Predicting extrapyramidal side effects in humans
20120 citationsauthor #6
Phosphodiesterase 9A Regulates Central cGMP and Modulates Responses to Cholinergic and Monoaminergic Perturbation In Vivo
201284 citationsauthor #7
Pharmacokinetic-Pharmacodynamic Modeling of the D2 and 5-HT2A Receptor Occupancy of Risperidone and Paliperidone in Rats
20120 citationsauthor #6
Translation of receptor occupancy measurements across species for an α 4 β 2 nAChR partial agonist
20110 citationsauthor #6
Quantitative PK–PD Model-Based Translational Pharmacology of a Novel Kappa Opioid Receptor Antagonist Between Rats and Humans
201140 citationsauthor #9
Pharmacological Characterization of 2-Methyl- N -((2 (cid:1) -(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a High-Affinity Antagonist Selective for (cid:1) -Opioid Receptors □ S
20110 citationsauthor #1
P2‐004: Donepezil causes acute increases in regional cerebral blood flow in normal rat
20110 citationsauthor #4
Duration of Action of a Broad Range of Selective κ-Opioid Receptor Antagonists Is Positively Correlated with c-Jun N-Terminal Kinase-1 Activation
2011114 citationsauthor #7
P3‐430: Gene and cell therapy approaches for prion diseases
20113 citationsauthor #1
Mechanism-Based Pharmacokinetic–Pharmacodynamic Modeling of the Dopamine D2 Receptor Occupancy of Olanzapine in Rats
201123 citationsauthor #6
Predicting dopamine D2 receptor occupancy in humans using a physiology-based approach
20110 citationsauthor #6
Pharmacological Characterization of 2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a High-Affinity Antagonist Selective for κ-Opioid Receptors
201158 citationsauthor #1
Pharmacokinetics, safety and tolerability of PF-04995274: A 5HT4 partial agonist being developed for the treatment of Alzheimer's disease
20113 citationsauthor #6
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
201144 citationsauthor #9
Predictive performance of two PK-PD models of D2 receptor occupancy of the antipsychotics risperidone and paliperidone in rats
20100 citationsauthor #7
ANALYTICAL CHALLENGES IN THE DEVELOPMENT OF A QUANTITATIVE SPE/LC/MS/MS ASSAY FOR AMYLOID BETA PEPTIDES IN CEREBROSPINAL FLUID
20102 citationsauthor #5
3′‐(Arylmethyl)‐ and 3′‐(Aryloxy)‐3‐phenyl‐4‐hydroxyquinolin‐2(1H)‐ ones: Orally Active Antagonists of the Glycine Site on the NMDA Receptor.
201015 citationsauthor #11
P3‐315: Significant reduction of brain and CSF amyloid‐β in mice following acute administration of a brain‐penetrant BACE1 inhibitor
20100 citationsauthor #10
Evaluation of a mechanism-based pharmacokinetic-pharmacodynamic model for D2 receptorb occupancy of olanzapine in rats
20101 citationsauthor #7
P2‐240: PF‐04447943, a novel PDE9A inhibitor, increases cGMP levels in cerebrospinal fluid: Translation from non‐clinical species to healthy human volunteers
200926 citationsauthor #8
Target site occupancy: emerging generalizations from clinical and preclinical studies.
2009120 citationsauthor #1
P1‐031: [3H]DAA1106 binding to hippocampal peripheral benzodiazepine receptors in kainic acid‐treated Tg2576 and C57BL6 mice
20090 citationsauthor #8
P.1.d.009 Asenapine: a translational analysis of receptor occupancy in human and rat brain with therapeutic implications
20082 citationsauthor #2
Validation of a rat in vivo [(3)H]M100907 binding assay to determine a translatable measure of 5-HT(2A) receptor occupancy.
200828 citationsauthor #11
Nucleus accumbens NMDA receptor subunit expression and function is enhanced in morphine-dependent rats.
200749 citationsauthor #3
Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor.
200516 citationsauthor #1
Assembly of N-methyl-D-aspartate (NMDA) receptors.
200342 citationsauthor #4
Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.
200332 citationsauthor #5
The effect of (+/-)-CP-101,606, an NMDA receptor NR2B subunit selective antagonist, in the Morris watermaze.
200345 citationsauthor #4
Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening.
200381 citationsauthor #6
N‐Methyl‐d‐aspartate receptor subtype‐selectivity of homoquinolinate: an electrophysiological and radioligand binding study using both native and recombinant receptors
20027 citationsauthor #1
Identification of Molecular Determinants That Are Important in the Assembly of N-Methyl-d-aspartate Receptors*
2001123 citationsauthor #3
Modulation of [3H]MK-801 binding to NMDA receptors in vivo and in vitro.
200056 citationsauthor #8
Characterisation of N‐Methyl‐D‐Aspartate Receptor‐Specific [3H]Ifenprodil Binding to Recombinant Human NR1a/NR2B Receptors Compared with Native Receptors in Rodent Brain Membranes
200043 citationsauthor #1
Delineation of the Structural Determinants of the N‐Methyl‐D‐Aspartate Receptor Glycine Binding Site
19992 citationsauthor #2
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
1997136 citationsauthor #11
4‐Substituted‐3‐phenylquinolin‐2(1H)‐ones: Acidic and Nonacidic Glycine Site N‐Methyl‐D‐aspartate Antagonists with in vivo Activity.
19975 citationsauthor #9
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
199753 citationsauthor #9
Generation and Characterisation of Stable Cell Lines Expressing Recombinant Human N‐Methyl‐d‐Aspartate Receptor Subtypes
199649 citationsauthor #1
Modulation of 45Ca2+ Influx into Cells Stably Expressing Recombinant Human NMDA Receptors by Ligands Acting at Distinct Recognition Sites
199653 citationsauthor #1
Synthesis and Structure‐Activity Relationships of Diiodotyrosine‐ Derived Glycine‐Site N‐Methyl‐D‐aspartate Receptor Ligands.
19960 citationsauthor #7
Synthesis and SAR of diiodotyrosine-derived glycine-site N-methyl-D-aspartate receptor ligands
19965 citationsauthor #7
CHARACTERIZATION OF STABLY EXPRESSED RECOMBINANT HUMAN N-METHYL-D-ASPARTATE RECEPTORS USING A CA-45(2+)-INFLUX ASSAY
19950 citationsauthor #1
5,6,7,8-Tetrahydroquinolones as antagonists at the glycine site of the NMDA receptor
199513 citationsauthor #3
Recombinant Human NMDA Homomeric NR1 Receptors Expressed in Mammalian Cells Form a High‐Affinity Glycine Antagonist Binding Site
199571 citationsauthor #1
Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists.
199533 citationsauthor #2
THE PHARMACOLOGICAL CHARACTERIZATION OF A STABLY TRANSFECTED CELL-LINE EXPRESSING HUMAN NMDAR1A/NMDAR2A RECEPTORS, USING RADIOLIGAND BINDING TECHNIQUES
19950 citationsauthor #1
Tetramic acids as novel glycine site antagonists
199516 citationsauthor #4
Polyamines modulate [3H]L-689,560 binding to the glycine site of the NMDA receptor from rat brain.
199414 citationsauthor #1
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically Active Anticonvulsants Acting by Antagonism at the Glycine Site of the N- Methyl-D-aspartate Receptor Complex.
19949 citationsauthor #12
3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors.
199371 citationsauthor #11
Anticonvulsant activity of glycine-site NMDA antagonists. 2. trans 2-carboxy-4-substituted tetrahydroquinolines.
199368 citationsauthor #10
Interactions Between the Glutamate and Glycine Recognition Sites of the N‐Methyl‐d‐Aspartate Receptor from Rat Brain, as Revealed from Radioligand Binding Studies
199340 citationsauthor #1
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.
199280 citationsauthor #6
Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain.
199271 citationsauthor #4
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.
1992166 citationsauthor #10
2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity.
199211 citationsauthor #3
The pharmacological specificity of N‐methyl‐d‐aspartate receptors in rat cerebral cortex: correspondence between radioligand binding and electrophysiological measurements
199126 citationsauthor #1

TIMELINE

1991 26 citations

1992 328 citations

1993 179 citations

1994 23 citations

1995 133 citations

1996 107 citations

1997 194 citations

1999 2 citations

2000 99 citations

2001 123 citations

2002 7 citations

2003 200 citations

2005 16 citations

2007 49 citations

2008 30 citations

2009 146 citations

2010 18 citations

2011 285 citations

2012 220 citations

2013 192 citations

2014 129 citations

2015 89 citations

2016 162 citations

2017 68 citations

2019 11 citations

2024 11 citations

S. Grimwood

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PAPERS

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