Results 81 to 90 of about 6,065 (241)

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +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

In silico investigations of the ionotropic cannabinoid receptor TRPV1 [PDF]

, 2022
Whether caused by inflammation or dysfunctional nerves, chronic pain affects nearly 10% of the world’s population. Since there are few treatments that are effective while being noninvasive and non-addictive, new targets are being explored.
Muller, Chante, NC DOCKS at The University of North Carolina at Greensboro   +1 more
core  

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Synthesis and Pharmacological Evaluation of 1-Phenyl‑3-Thiophenylurea Derivatives as Cannabinoid Type‑1 Receptor Allosteric Modulators

, 2019
We previously reported diarylurea derivatives as cannabinoid type-1 receptor (CB1) allosteric modulators, which were effective in attenuating cocaine-seeking behavior.
Thuy Nguyen (160049), Thomas F. Gamage (4376248), Yanan Zhang (1322391), Ann M. Decker (1322412), Tiffany L. Langston (4341676), Daniel Barrus (7541399), Jun-Xu Li (1618639), Brian F. Thomas (1322394)   +7 more
core   +3 more sources

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

Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways

British Journal of Pharmacology, EarlyView.
Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck, Mario van der Stelt   +1 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

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

5‐HT2A receptor agonism by tert‐leucinamide and valinamide synthetic cannabinoids: In vitro and in vivo evidence

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose New synthetic cannabinoid receptor agonists (SCRAs) are associated with severe adverse effects, including unexpected psychiatric symptoms. These compounds are mainly active through their potent agonism on the cannabinoid receptors CB1 and CB2.
Giorgia Corli, Deborah Rudin, Dino Luethi, Matthias E. Liechti, Sabrine Bilel, Matteo Marti, Henrik Green, Manuela Carla Monti, Caitlyn Norman   +8 more
wiley   +1 more source