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Biased mu-opioid receptor ligands: a promising new generation of pain therapeutics

Current opinion in pharmacology, 2017-02, Vol.32, p.77-84

2017

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Quantifying ligand bias at seven-transmembrane receptors

Molecular pharmacology, 2011-09, Vol.80 (3), p.367-377

2011

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Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance

The Journal of pharmacology and experimental therapeutics, 2010-12, Vol.335 (3), p.572-579

2010

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Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

Journal of medicinal chemistry, 2013-10, Vol.56 (20), p.8019-8031

2013

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Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR)

The Journal of biological chemistry, 2014-05, Vol.289 (20), p.14211-14224

2014

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TRV0109101, a G Protein-Biased Agonist of the µ -Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration

The Journal of pharmacology and experimental therapeutics, 2017-08, Vol.362 (2), p.254-262

2017

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Evidence for allosteric interactions of antagonist binding to the smoothened receptor

The Journal of pharmacology and experimental therapeutics, 2009-06, Vol.329 (3), p.995-1005

2009

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Biased ligands: pathway validation for novel GPCR therapeutics

Current opinion in pharmacology, 2014-06, Vol.16, p.108-115

2014

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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine

The Journal of pharmacology and experimental therapeutics, 2013-03, Vol.344 (3), p.708-717

2013

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Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret

Drug metabolism and disposition, 2008-09, Vol.36 (9), p.1846-1852

2008

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Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors

The Journal of biological chemistry, 2000-11, Vol.275 (44), p.34086-34091

2000

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Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies

The Journal of pharmacology and experimental therapeutics, 1998-07, Vol.286 (1), p.459

1998

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Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors

The Journal of pharmacology and experimental therapeutics, 2003-04, Vol.305 (1), p.57

2003

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Quantifying Ligand Bias at Seven-Transmembrane ReceptorsS

Molecular pharmacology, 2011-09, Vol.80 (3), p.367-377

2011

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TRV120027, a β-Arrestin Biased Ligand at the Angiotensin II Type 1 Receptor, Produces Unique Pharmacology and Is a Novel Potential Therapy for Heart Failure

Journal of cardiac failure, 2010, Vol.16 (8), p.S72-S72

2010

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Pharmacological Characterization of a Novel Nonpeptide Antagonist Radioligand, (±) -N -[2-Methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1 H -1,2,3-triazolo[4,5- c ]pyridin-4-amine ([ 3 H]SN003) for Corticotropin-Releasing Factor 1 Receptors

The Journal of pharmacology and experimental therapeutics, 2003-04, Vol.305 (1), p.57-69

2003

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Novel receptor site involved in enhancement of stimulus-induced acetylcholine, dopamine, and serotonin release

Molecular pharmacology, 1991-07, Vol.40 (1), p.16-21

1991

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Presenilin-1 and -2 Are Molecular Targets for Î³-Secretase Inhibitors

The Journal of biological chemistry, 2000-11, Vol.275 (44), p.34086

2000

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Somatic Mutations in UBA1 and Severe Adult-Onset Autoinflammatory Disease

The New England journal of medicine, 2020-12, Vol.383 (27), p.2628-2638

2020

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Global determinants of insect mitochondrial genetic diversity

Nature communications, 2023-08, Vol.14 (1), p.5276-5276, Article 5276

2023

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GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

Clinical cancer research, 2011-03, Vol.17 (5), p.989-1000

2011

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Improved longitudinal [18F]-AV45 amyloid PET by white matter reference and VOI-based partial volume effect correction

NeuroImage (Orlando, Fla.), 2015-03, Vol.108, p.450-459

2015

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Metabolic partitioning across individuals in ecological communities

Global ecology and biogeography, 2017-09, Vol.26 (9/10), p.993-997

2017

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Accurate population estimation of Caprinae using camera traps and distance sampling

Scientific reports, 2020-10, Vol.10 (1), p.17729-17729, Article 17729

2020

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Biased mu-opioid receptor ligands: a promising new generation of pain therapeutics

Quantifying ligand bias at seven-transmembrane receptors

Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance

Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR)

TRV0109101, a G Protein-Biased Agonist of the µ -Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration

Evidence for allosteric interactions of antagonist binding to the smoothened receptor

Biased ligands: pathway validation for novel GPCR therapeutics

A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine

Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret

Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors

Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies

Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors

Quantifying Ligand Bias at Seven-Transmembrane ReceptorsS

TRV120027, a β-Arrestin Biased Ligand at the Angiotensin II Type 1 Receptor, Produces Unique Pharmacology and Is a Novel Potential Therapy for Heart Failure

Pharmacological Characterization of a Novel Nonpeptide Antagonist Radioligand, (±) -N -[2-Methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1 H -1,2,3-triazolo[4,5- c ]pyridin-4-amine ([ 3 H]SN003) for Corticotropin-Releasing Factor 1 Receptors

Novel receptor site involved in enhancement of stimulus-induced acetylcholine, dopamine, and serotonin release

Presenilin-1 and -2 Are Molecular Targets for Î³-Secretase Inhibitors

Somatic Mutations in UBA1 and Severe Adult-Onset Autoinflammatory Disease

Loss of TREM2 function increases amyloid seeding but reduces plaque-associated ApoE

Global determinants of insect mitochondrial genetic diversity

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

Improved longitudinal [18F]-AV45 amyloid PET by white matter reference and VOI-based partial volume effect correction

Metabolic partitioning across individuals in ecological communities

Accurate population estimation of Caprinae using camera traps and distance sampling

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