Results 41 to 50 of about 1,820,241 (196)

Innovative Approach Reveals How Receptors Control G Protein State Equilibria

Advanced Science, EarlyView.
Using conformational specific trFRET biosensors of the Gi protein (depicted at the bottom), the authors show that receptor activation can not only release GDP from the inactive G protein, but can also release GTP from the activated G protein, leading to the reformation of the RG ternary complex.
Alexandre Bouyssou, Mélanie Da Silva, Julien Soulé, Ludovic Fabre, Laurent Lamarque, Rémy Sounier, Thierry Durroux, Sébastien Granier, Thomas Roux, Elodie Dupuis, Eric Trinquet, Philippe Rondard, Jean‐Philippe Pin   +12 more
wiley   +1 more source

Effects of Central Administration of Opioid Peptides, Vasotocin, Mesotocin, and Corticotrophin-Releasing Factor on Water Intake in Chicks

The Journal of Poultry Science
Freedom from thirst is an undeniable requirement of the poultry industry. However, the regulatory mechanisms underlying water intake in chicks are not yet fully understood.
Yuhui Zhang, Kaoruko Murata, Junya Takegaki, Takaoki Saneyasu, Kazuhisa Honda   +4 more
doaj   +1 more source

EphB1 Receptor Blockade Augments Morphine Antinociception via Inhibiting GRK2‐Mediated µ‐Opioid Receptor Internalization

Advanced Science, EarlyView.
Administration of opioids activates ephrinB2‐EphB1 receptor signaling. Activated EphB1 receptors induce GRK2‐mediated phosphorylation of MOR at Ser375, which initiates the internalization of MOR and reduces opioid antinociception at the behavioral level. ABSTRACT Opioids are the primary treatment for severe pain in clinical practice.
Bo Peng, Xiaqing Lin, Hongyu Yao, Cheng Li, Huabao Liao, Yuexin Liu, Boxu Cao, Xue‑Jun Song   +7 more
wiley   +1 more source

A Novel Acetylated Analogue of Dynorphin A-(1−11) Amide as a κ-Opioid Receptor Antagonist

, 2016
A Novel Acetylated Analogue of Dynorphin A-(1−11) Amide as a κ-Opioid Receptor ...
Qiang Wan (211695), Jane V. Aldrich (2332483), Thomas F. Murray (776850)   +2 more
core   +1 more source

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)‐VK4‐116, as a Non‐Opioid Medication for the Treatment of Opioid Use Disorder

Medicinal Research Reviews, EarlyView.
ABSTRACT Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor‐targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions
Chia‐Kuei Wu, Yu‐Chih Lin, Junfeng Huang, Bangwei Ding, Pramod Terse, Rahul Nandre, Haksong Jin, Molly Congdon, Kun Shen, Philip Sanderson, Gregory Tawa, Stephanie Mounaud, Marta De Santis, Donald Lo, Elizabeth A. Ottinger, Amy Hauck Newman   +15 more
wiley   +1 more source

Stilbenes as κ‑Selective, Non-nitrogenous Opioid Receptor Antagonists

, 2015
The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the κ receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features.
John A. Beutler (7678), Alyssa M. Hartung (1309665), David F. Wiemer (1309671), Hernán A. Navarro (1309674), Jeffrey D. Neighbors (1309668)   +4 more
core   +1 more source

Opioid receptor agonist–antagonists in pain management: receptor specific mechanisms, dose response relationships, and clinical combination strategies

Frontiers in Pain Research
Opioid receptor agonist–antagonists occupy a distinctive position between high-efficacy agonists and pure antagonists and have been widely used in clinical pain management.
Sining Zhao, Sining Zhao, Zhiqiang Xue, Shu Wang   +3 more
doaj   +1 more source

A Chimeric Analysis of the Opioid Receptor Domains Critical for the Binding Selectivity of μ Opioid Ligands

Neurobiology of Disease, 1996
The μ opioid receptor plays a key role in mediating the physiological, pharmacological, and behavioral effects of endogenous opioids and of opiate drugs such as morphine and heroin.
Brendon Watson, Fan Meng, Huda Akil
doaj   +1 more source

Repurposing antimicrobial agents for neuroprotection: Mechanisms, clinical potential, and challenges

Neuroprotection, EarlyView.
Antimicrobial agents exert neuroprotective effects through modulation of interconnected pathways. Tetracyclines, macrolides, antimalarial agents, sulfones, and antiparasitic agents suppress neuroinflammation, oxidative stress, and apoptosis while preserving mitochondrial function and neurotransmission.
Mohammad Amin Manavi, Mohammadreza Salehi, Razieh Mohammad Jafari, Ramin Goudarzi, Saman Khosravi, Ahmad Reza Dehpour   +5 more
wiley   +1 more source

Presynaptic Mechanism for Anti-Analgesic and Anti-Hyperalgesic Actions of κ-Opioid Receptors

, 2003
Glutamate neurotransmission plays an important role in the processing of pain and in chronic opioid-induced neural and behavioral plasticity, such as opioid withdrawal and opioid dependence.
Zhizhong Z. Pan, Bihua Bie
core   +1 more source