Search results for: John R. Traynor

Items from 1 to 20 out of 58 results

article

Opioid research in the time of the opioid crisis

John R. Traynor, Jose A. Moron

British Journal of Pharmacology > 180 > 7 > 793 - 796

LINKED ARTICLES This article is part of a themed issue on Advances in Opioid Pharmacology at the Time of the Opioid Epidemic. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v180.7/issuetoc

article

Mixed‐solvent molecular dynamics simulation‐based discovery of a putative allosteric site on regulator of G protein signaling 4

Wallace K. B. Chan, Debarati DasGupta, Heather A. Carlson, John R. Traynor

Journal of Computational Chemistry > 42 > 30 > 2170 - 2180

Regulator of G protein signaling 4 (RGS4) is an intracellular protein that binds to the G_α subunit ofheterotrimeric G proteins and aids in terminating G protein coupled receptor signaling. RGS4 has been implicated in pain, schizophrenia, and the control of cardiac contractility. Inhibitors of RGS4 have been developed but bind covalently to cysteine residues on the protein. Therefore, we sought to...

article

The δ‐opioid receptor positive allosteric modulator BMS 986187 is a G‐protein‐biased allosteric agonist

M. Alexander Stanczyk, Kathryn E. Livingston, Louise Chang, Zara Y. Weinberg, more

British Journal of Pharmacology > 176 > 11 > 1649 - 1663

Background and Purpose The δ‐opioid receptor is an emerging target for the management of chronic pain and depression. Biased signalling, the preferential activation of one signalling pathway over another downstream of δ‐receptors, may generate better therapeutic profiles. BMS 986187 is a positive allosteric modulator of δ‐receptors. Here, we ask if BMS 986187 can directly activate the receptor from...

article

Allostery at opioid receptors: modulation with small molecule ligands

Kathryn E Livingston, John R Traynor

British Journal of Pharmacology > 175 > 14 > 2846 - 2856

Opioid receptors are 7‐transmembrane domain receptors that couple to heterotrimeric G proteins. The endogenous ligands for opioid receptors are peptides which bind to the orthosteric site on the receptors. The μ‐opioid receptor is the target for opioid analgesics, while the δ‐opioid receptor has been suggested as a target for pain management, migraine and depression. Similarly, κ‐opioid receptors...

article

In vivo effects of μ‐opioid receptor agonist/δ‐opioid receptor antagonist peptidomimetics following acute and repeated administration

Jessica P Anand, Kelsey E Kochan, Anthony F Nastase, Deanna Montgomery, more

British Journal of Pharmacology > 175 > 11 > 2013 - 2027

Background and Purpose Agonists at μ‐opioid receptors (μ‐receptors) are used for pain management but produce adverse effects including tolerance, dependence and euphoria. The co‐administration of a μ‐receptor agonist with a δ‐opioid receptor (δ‐receptor) antagonist has been shown to produce antinociception with reduced development of some side effects. We characterized the effects of three μ‐receptor...

article

Role of signalling molecules in behaviours mediated by the δ opioid receptor agonist SNC80

Isaac J Dripps, Brett T Boyer, Richard R Neubig, Kenner C Rice, more

British Journal of Pharmacology > 175 > 6 > 891 - 901

Background and Purpose GPCRs exist in multiple conformations that can engage distinct signalling mechanisms which in turn may lead to diverse behavioural outputs. In rodent models, activation of the δ opioid receptor (δ‐receptor) has been shown to elicit antihyperalgesia, antidepressant‐like effects and convulsions. We recently showed that these δ‐receptor‐mediated behaviours are differentially regulated...

article

Role of the guanine nucleotide binding protein, Gα_o, in the development of morphine tolerance and dependence

Jennifer T. Lamberts, Lisa D. Rosenthal, Emily M. Jutkiewicz, John R. Traynor

Psychopharmacology > 2018 > 235 > 1 > 71-82

Rationale The use of morphine and other opioids for chronic pain is limited by the development of analgesic tolerance and physical dependence. Morphine produces its effects by activating the μ opioid receptor, which couples to Gα_i/o-containing heterotrimeric G proteins. Evidence suggests that the antinociceptive effects of morphine are mediated by Gα_o. However, the role of Gα_o in the development of...

article

Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study

Phong M. Truong, Sergio A. Hassan, Yong-Sok Lee, Theresa A. Kopajtic, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 8 > 2406-2422

The enantiomers of a variety of N-alkyl-, N-aralkyl-, and N-cyclopropylalkyl-9β-hydroxy-5-(3-hydroxyphenyl)morphans were synthesized employing cyanogen bromide and K₂CO₃ to improve the original N-demethylation procedure. Their binding affinity to the μ-, δ-, and κ-opioid receptors (ORs) was determined and functional (GTP_γ³⁵S) assays were carried out on those with reasonable affinity. The 1R,5R,9S-enantiomers...

article

Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands

Jason R. Healy, Padmavani Bezawada, Nicholas W. Griggs, Andrea L. Devereaux, more

Bioorganic & Medicinal Chemistry Letters > 2017 > 27 > 3 > 666-669

Opioid analgesic tolerance remains a considerable drawback to chronic pain management. The finding that concomitant administration of delta opioid receptor (DOR) antagonists attenuates the development of tolerance to mu opioid receptor (MOR) agonists has led to interest in producing bifunctional MOR agonist/DOR antagonist ligands. Herein, we present 7-benzylideneoxymorphone (6, UMB 246) displaying...

article

The role of regulator of G protein signaling 4 in delta-opioid receptor-mediated behaviors

Isaac J. Dripps, Qin Wang, Richard R. Neubig, Kenner C. Rice, more

Psychopharmacology > 2017 > 234 > 1 > 29-39

Rationale Regulator of G protein signaling (RGS) proteins act as negative modulators of G protein signaling. RGS4 has been shown to negatively modulate G protein signaling mediated by the delta opioid receptor (DOPr) in vitro. However, the role of RGS4 in modulating DOPr-mediated behaviors in vivo has not been elucidated. Objective The aim of this study was to compare the ability of the DOPr agonist...

article

Dynamic Coupling and Allosteric Networks in the Alpha Subunit of Heterotrimeric G Proteins

Xin-Qiu Yao, Rabia Malik, Nicholas W. Griggs, Lars Skjærven, more

Biophysical Journal > 2016 > 110 > 3 Supplement 1 > 427a

article

Nucleus accumbens shell excitability is decreased by methamphetamine self-administration and increased by 5-HT2C receptor inverse agonism and agonism

Steven M. Graves, Mary J. Clark, John R. Traynor, Xiu-Ti Hu, more

Neuropharmacology > 2015 > 89 > Complete > 113-121

Methamphetamine profoundly increases brain monoamines and is a widely abused psychostimulant. The effects of methamphetamine self-administration on neuron function are not known for the nucleus accumbens, a brain region involved in addictive behaviors, including drug-seeking. One therapeutic target showing preclinical promise at attenuating psychostimulant-seeking is 5-HT _2C receptors; however,...

article

Challenges for opioid receptor nomenclature: IUPHAR Review 9

Brian M Cox, Macdonald J Christie, Lakshmi Devi, Lawrence Toll, more

British Journal of Pharmacology > 172 > 2 > 317 - 323

Recent developments in the study of the structure and function of opioid receptors raise significant challenges for the definition of individual receptor types and the development of a nomenclature that precisely describes isoforms that may subserve different functions in vivo. Presentations at the 2013 meeting of the International Narcotics Research Conference in Cairns, Australia, considered some...

article

5-HT1A receptor-mediated phosphorylation of extracellular signal-regulated kinases (ERK1/2) is modulated by regulator of G protein signaling protein 19

Qin Wang, Akiko Terauchi, Christopher H. Yee, Hisashi Umemori, more

Cellular Signalling > 2014 > 26 > 9 > 1846-1852

The 5-HT1A receptor is a G protein coupled receptor (GPCR) that activates G proteins of the Gαi/o family. 5-HT1A receptors expressed in the raphe, hippocampus and prefrontal cortex are implicated in the control of mood and are targets for anti-depressant drugs. Regulators of G protein signaling (RGS) proteins are members of a large family that play important roles in signal transduction downstream...

article

Synergistic activity between the delta-opioid agonist SNC80 and amphetamine occurs via a glutamatergic NMDA-receptor dependent mechanism

Kelly E. Bosse, Emily M. Jutkiewicz, Kristin N. Schultz-Kuszak, Omar S. Mabrouk, more

Neuropharmacology > 2014 > 77 > Complete > 19-27

Glutamate is known to cause the release of dopamine through a Ca ²⁺ -sensitive mechanism that involves activation of NMDA ionotropic glutamate receptors. In the current study, we tested the hypothesis that the delta opioid agonist SNC80 acts indirectly, via the glutamatergic system, to enhance both amphetamine-stimulated dopamine efflux from striatal preparations and amphetamine-stimulated...

article

Translation of structure‐activity relationships from cyclic mixed efficacy opioid peptides to linear analogues

Jessica P. Anand, Vanessa R. Porter‐Barrus, Helen V. Waldschmidt, Larisa Yeomans, more

Biopolymers > 102 > 1 > 107 - 114

Most opioid analgesics used in the treatment of pain are mu opioid receptor (MOR) agonists. While effective, there are significant drawbacks to opioid use, including the development of tolerance and dependence. However, the coadministration of a MOR agonist with a delta opioid receptor (DOR) antagonist slows the development of MOR‐related side effects, while maintaining analgesia. We have previously...

article

Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands

Aaron M. Bender, Mary J. Clark, Michael P. Agius, John R. Traynor, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 2 > 548-551

In this letter, we describe a series of 4-substituted piperidine and piperazine compounds based on tetrahydroquinoline 1, a compound that shows balanced, low nanomolar binding affinity for the mu opioid receptor (MOR) and the delta opioid receptor (DOR). We have shown that by changing the length and flexibility profile of the side chain in this position, binding affinity is improved at both receptors...

article

Modulation of Opioid Receptor Ligand Affinity and Efficacy Using Active and Inactive State Receptor Models

Jessica P. Anand, Lauren C. Purington, Irina D. Pogozheva, John R. Traynor, more

Chemical Biology & Drug Design > 80 > 5 > 763 - 770

Mu opioid receptor (MOR) agonists are widely used for the treatment of pain; however, chronic use results in the development of tolerance and dependence. It has been demonstrated that coadministration of a MOR agonist with a delta opioid receptor (DOR) antagonist maintains the analgesia associated with MOR agonists, but with reduced negative side‐effects. Using our newly refined opioid receptor models...

article

Development and in Vitro Characterization of a Novel Bifunctional μ-Agonist/δ-Antagonist Opioid Tetrapeptide

Lauren C. Purington, Katarzyna Sobczyk-Kojiro, Irina D. Pogozheva, John R. Traynor, more

ACS Chemical Biology > 2011 > 6 > 12 > 1375 - 1381

article

Regulators of G Protein Signaling (RGS) Proteins as Drug Targets: Modulating G-Protein-Coupled Receptor (GPCR) Signal Transduction

David L. Roman, John R. Traynor

Journal of Medicinal Chemistry > 2011 > 54 > 21 > 7433 - 7440

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Search results for: John R. Traynor

Opioid research in the time of the opioid crisis

Mixed‐solvent molecular dynamics simulation‐based discovery of a putative allosteric site on regulator of G protein signaling 4

The δ‐opioid receptor positive allosteric modulator BMS 986187 is a G‐protein‐biased allosteric agonist

Allostery at opioid receptors: modulation with small molecule ligands

In vivo effects of μ‐opioid receptor agonist/δ‐opioid receptor antagonist peptidomimetics following acute and repeated administration

Role of signalling molecules in behaviours mediated by the δ opioid receptor agonist SNC80

Role of the guanine nucleotide binding protein, Gα_o, in the development of morphine tolerance and dependence

Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study

Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands

The role of regulator of G protein signaling 4 in delta-opioid receptor-mediated behaviors

Dynamic Coupling and Allosteric Networks in the Alpha Subunit of Heterotrimeric G Proteins

Nucleus accumbens shell excitability is decreased by methamphetamine self-administration and increased by 5-HT2C receptor inverse agonism and agonism

Challenges for opioid receptor nomenclature: IUPHAR Review 9

5-HT1A receptor-mediated phosphorylation of extracellular signal-regulated kinases (ERK1/2) is modulated by regulator of G protein signaling protein 19

Synergistic activity between the delta-opioid agonist SNC80 and amphetamine occurs via a glutamatergic NMDA-receptor dependent mechanism

Translation of structure‐activity relationships from cyclic mixed efficacy opioid peptides to linear analogues

Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands

Modulation of Opioid Receptor Ligand Affinity and Efficacy Using Active and Inactive State Receptor Models

Development and in Vitro Characterization of a Novel Bifunctional μ-Agonist/δ-Antagonist Opioid Tetrapeptide

Regulators of G Protein Signaling (RGS) Proteins as Drug Targets: Modulating G-Protein-Coupled Receptor (GPCR) Signal Transduction

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