Results 91 to 100 of about 5,036 (195)

Divergence in μ and δ opioid receptor pharmacology in neurons and antinociceptive efficacy in neuropathic pain: Insights from MP135 and CYM51010

British Journal of Pharmacology, Volume 183, Issue 10, Page 2307-2323, May 2026.
Background and purpose Opioids targeting the μ opioid receptor remain largely ineffective in neuropathic pain conditions, emphasizing the need for novel therapeutic strategies. MP135 was reported to reduce thermal nociception in naive animals by activating μ‐δ opioid receptor heteromers.
Perrine Inquimbert, Chantal Fitterer, Sylvain Hugel, Mila Jesic, Yannick Goumon, Virgine Andry, Severine Schneider, Francois Daubeuf, Abdelfattah Faouzi, Stephane Doridot, Susruta Majumdar, Frederic Bihel, Martine Schmitt, Dominique Massotte   +13 more
wiley   +1 more source

Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models

, 2018
G protein-gated inwardly rectifying potassium (GIRK) channels are potassium-selective ion channels. As their name suggests, GIRK channels are effectors of Gi/o G protein-couple receptors whereby activation of these GPCRs leads to increased GIRK channel ...
Craig W. Linsdley (6069560), C. David Weaver (655503), Ryan D. Morrison (1339743), Thomas M. Bridges (1336731), Carrie K. Jones (1326210), Corey R. Hopkins (147168), Kevin Wickman (477695), Michael Bubser (1334478), J. Scott Daniels (1326204), Kristopher K. Abney (6069557), Krystian A. Kozek (2071033), Yu Du (618167)   +11 more
core   +1 more source

Feedback control of excitability and high K+ induced epileptiform bursts in male rat hippocampal slices with a photocaged adenosine A1 receptor agonist

British Journal of Pharmacology, Volume 183, Issue 10, Page 2578-2591, May 2026.
Background and Purpose Adenosine is a potent regulator of neurotransmission and neuronal excitability, through activation of Gi coupled adenosine A1 receptors (A1Rs). Adenosine has gained interest as an anticonvulsant because of its endogenous involvement in ending seizure activity, but peripheral side effects require local application.
Erine Craey, Marijke Vergaelen, Serge Van Calenbergh, Jeroen Spanoghe, Evelien Carrette, Kristl Vonck, Paul Boon, Wytse J. Wadman, Robrecht Raedt   +8 more
wiley   +1 more source

GIRK2 splice variants and neuronal G protein-gated K+ channels: implications for channel function and behavior

Scientific Reports, 2017
Many neurotransmitters directly inhibit neurons by activating G protein-gated inwardly rectifying K+ (GIRK) channels, thereby moderating the influence of excitatory input on neuronal excitability. While most neuronal GIRK channels are formed by GIRK1 and
Ezequiel Marron Fernandez de Velasco, Lei Zhang, Baovi N. Vo, Megan Tipps, Shannon Farris, Zhilian Xia, Allison Anderson, Nicholas Carlblom, C. David Weaver, Serena M. Dudek, Kevin Wickman   +10 more
doaj   +1 more source

Distinct regulation of dopamine D2S and D2L autoreceptor signaling by calcium

eLife, 2015
D2 autoreceptors regulate dopamine release throughout the brain. Two isoforms of the D2 receptor, D2S and D2L, are expressed in midbrain dopamine neurons. Differential roles of these isoforms as autoreceptors are poorly understood.
Stephanie C Gantz, Brooks G Robinson, David C Buck, James R Bunzow, Rachael L Neve, John T Williams, Kim A Neve   +6 more
doaj   +1 more source

G-Protein-Coupled Inwardly Rectifying Potassium (GIRK) Channel Activation by the p75 Neurotrophin Receptor Is Required for Amyloid β Toxicity

Frontiers in Neuroscience, 2017
Alzheimer's disease is characterized by cognitive decline, neuronal degeneration, and the accumulation of amyloid-beta (Aβ). Although, the neurotoxic Aβ peptide is widely believed to trigger neuronal dysfunction and degeneration in Alzheimer's disease ...
Linda M. May, Victor Anggono, Victor Anggono, Helen M. Gooch, Se E. Jang, Se E. Jang, Dusan Matusica, Dusan Matusica, Georg M. Kerbler, Frederic A. Meunier, Frederic A. Meunier, Pankaj Sah, Elizabeth J. Coulson, Elizabeth J. Coulson, Elizabeth J. Coulson   +14 more
doaj   +1 more source

Cholesterol-Binding Sites in GIRK Channels: The Devil is in the Details [PDF]

Lipid Insights, 2018
In recent years, it has become evident that cholesterol plays a direct role in the modulation of a variety of ion channels. In most cases, cholesterol downregulates channel activity. In contrast, our earlier studies have demonstrated that atrial G protein inwardly rectifying potassium (GIRK) channels are upregulated by cholesterol.
openaire   +2 more sources

The K+ channel GIRK2 is both necessary and sufficient for peripheral opioid‐mediated analgesia

EMBO Molecular Medicine, 2013
The use of opioid agonists acting outside the central nervous system (CNS) is a promising therapeutic strategy for pain control that avoids deleterious central side effects such as apnea and addiction.
Dinah Nockemann, Morgane Rouault, Dominika Labuz, Philip Hublitz, Kate McKnelly, Fernanda C. Reis, Christoph Stein, Paul A. Heppenstall   +7 more
doaj   +1 more source

Modulation of Basal and Receptor-Induced GIRK Potassium Channel Activity and Neuronal Excitability by the Mammalian PINS Homolog LGN [PDF]

, 2006
SummaryG protein-activated inwardly rectifying potassium (GIRK) channels mediate slow synaptic inhibition and control neuronal excitability. It is unknown whether GIRK channels are subject to regulation by guanine dissociation inhibitor (GDI) proteins ...
Roberts, Richard W., Qian, Xiang, Ja, William W., Wiser, Ofer, Reuveny, Eitan, Jan, Yuh Nung, Jan, Lily Yeh, Ehlers, Melissa   +7 more
core   +1 more source

Die Rolle von Kir3.1- und Kir3.4- Untereinheiten in der Regulation kardialer GIRK-Kanäle in Vorhofmyozyten

, 2011
Cardiac GIRK channels are composed of Kir3.1 and Kir3.4 subunits and contribute to vagally induced bradycardia. Here, the effects of altered subunit expression ratios on cardiac GIRK currents were studied using adenovirally induced overexpression and RNA
Mintert-Jancke, Elisa (Dr. rer. nat.)
core   +1 more source