Results 71 to 80 of about 247,667 (242)

Inhibition of kynurenine 3‐monooxygenase (KMO) reduces fentanyl and sucrose intake and relapse‐like behaviour in rats

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Opioid use disorder, particularly involving fentanyl, poses major challenges due to high relapse rates and limited effectiveness of pharmacotherapies. The kynurenine pathway has emerged as a target for addiction treatment through its modulation of glutamatergic and dopaminergic neurotransmission.
Carlos Núñez‐de la Calle, Lluna Careaga, Stefanie Malan‐Müller, Álvaro del Río‐García, Yaiza Trueba, Leticia Gil de Biedma‐Elduayen, Nuria Morales‐Puerto, Rebeca Vidal, Åsa Wiman, Sophie Erhardt, María Dolores Gutiérrez‐López, Esther O'Shea, María Isabel Colado   +12 more
wiley   +1 more source

Cannabinoid Modulation of Excitability and Short-Term Neuronal Dynamics in the Dorsal and Ventral Hippocampus

Biology
Endocannabinoids, acting primarily through CB1 receptors, are critical modulators of neuronal activity, influencing cognitive functions and emotional processing.
Giota Tsotsokou, Ioanna-Maria Sotiropoulou, Klearchos Stampolitis, George D. Oikonomou, Aikaterini-Paraskevi Avdi, Costas Papatheodoropoulos   +5 more
doaj   +1 more source

Disordered Peptides Looking for Their Native Environment: Structural Basis of CB1 Endocannabinoid Receptor Binding to Pepcans

Frontiers in Molecular Biosciences, 2018
Endocannabinoid peptides, or “pepcans,” are endogenous ligands of the CB1 cannabinoid receptor. Depending on their length, they display diverse activity: For instance, the nona-peptide Pepcan-9, also known as hemopressin, is a powerful inhibitor of CB1 ...
Alessandro Emendato, Remo Guerrini, Erika Marzola, Hans Wienk, Rolf Boelens, Serena Leone, Delia Picone   +6 more
doaj   +1 more source

Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats

Pharmacology Research & Perspectives, 2014
The cannabinoid CB1 receptor system is involved in feeding behaviors and the CB1 receptor antagonist SR141716A is an effective antiobesity drug. However, SR141716A also has serious side effects, which prompted the exploration of alternative strategies to
Yuanyuan Ding, Y. Qiu, L. Jing, D. Thorn, Yanan Zhang, Jun-Xu Li   +5 more
semanticscholar   +1 more source

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Determination of the Cannabinoid CB1 Receptor’s Positive Allosteric Modulator Binding Site through Mutagenesis Studies

Pharmaceuticals
Positive allosteric modulators (PAMs) of the cannabinoid CB1 receptor (CB1) offer potential therapeutic advantages in the treatment of neuropathic pain and addiction by avoiding the adverse effects associated with orthosteric CB1 activation.
Hayley M. Green, Daniel M. J. Fellner, David B. Finlay, Daniel P. Furkert, Michelle Glass   +4 more
doaj   +1 more source

Cannabinoid CB1 allosteric ligands suppress inflammatory pain in male mice without tolerance, motor impairment, memory deficits or respiratory depression

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators (PAMs) engage sites distinct from the orthosteric CB1 cannabinoid receptor binding site. GAT211, a racemic ligand, contains GAT228 (R) and GAT229 (S) enantiomers. Whether enantiomer‐mediated differences in allosteric activation or positive allosteric modulation translate into differences in
Ifeoluwa D. Solomon, Sumanta Garai, Ganesh A. Thakur, Andrea G. Hohmann   +3 more
wiley   +1 more source

Mechanisms of Broad-Spectrum Antiemetic Efficacy of Cannabinoids against Chemotherapy-Induced Acute and Delayed Vomiting

Pharmaceuticals, 2010
Chemotherapy-induced nausea and vomiting (CINV) is a complex pathophysiological condition and consists of two phases. The conventional CINV neurotransmitter hypothesis suggests that the immediate phase is mainly due to release of serotonin (5-HT) from ...
Nissar A. Darmani
doaj   +1 more source

Positioning Incretin‐Based and Next‐Generation Obesity Management Medications: A Methodological Framework for a Series of Systematic Reviews and Network Meta‐Analyses

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Background The obesity pharmacotherapy landscape is evolving rapidly, with several approved incretin‐based therapies and an expanding pipeline of investigational compounds targeting multiple metabolic pathways. Conventional evidence syntheses often struggle to accommodate differences in dose selection, treatment duration and stage of clinical ...
Matteo Monami, Benedetta Ragghianti, Edoardo Mannucci   +2 more
wiley   +1 more source

Allosteric Modulation of a Cannabinoid G Protein-coupled Receptor

Journal of Biological Chemistry, 2013
Background: Cannabinoid-1 (CB1) receptor allosteric modulator ORG27569 increases CP55,940 binding, yet antagonizes G protein signaling. Results: ORG27569 binding sterically blocks movement in CB1 extracellular loops and transmembrane helix 6 (TMH6 ...
Derek M. Shore, G. Baillie, Dow H. Hurst, F. Navas, H. Seltzman, J. Marcu, M. Abood, R. Ross, P. Reggio   +8 more
semanticscholar   +1 more source