Results 71 to 80 of about 562,936 (248)

Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]

, 2013
CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Boros, Eszter, Hunyady, L., Gyombolai, Pál, Boros, E., Turu, G., Turu, Gábor, Gyombolai, P., Hunyady, László   +7 more
core   +1 more source

Allosteric modulators restore orthosteric agonist binding to mutated CB1 receptors

Journal of Pharmacy and Pharmacology, 2020
Abstract Objectives To determine if diminished orthosteric agonist binding due to mutations in extracellular loops 1 or 2 of the cannabinoid receptor 1 (CB1) can be overcome by an allosteric modulator and restore agonist binding. Methods
Rachel Dopart, Debra A Kendall
openaire   +3 more sources

Behavioral effects of the novel potent cannabinoid CB1 agonist AM 4054 [PDF]

Pharmacology Biochemistry and Behavior, 2013
Due to the ubiquity of the CB1 cannabinoid receptor throughout the nervous system, as well as the many potential therapeutic uses of CB1 agonist-based interventions, it is desirable to synthesize novel probes of the CB1 receptor. Here, the acute behavioral effects of systemic (i.p.) administration of the putative novel CB1 full agonist AM 4054 were ...
Peter J, McLaughlin, Ganesh A, Thakur, V Kiran, Vemuri, Evan D, McClure, Cara M, Brown, Keisha M, Winston, Jodianne T, Wood, Alexandros, Makriyannis, John D, Salamone   +8 more
openaire   +2 more sources

Expression and function of cannabinoid receptors CB1 and CB2 and their cognate cannabinoid ligands in murine embryonic stem cells. [PDF]

PLoS ONE, 2007
Characterization of intrinsic and extrinsic factors regulating the self-renewal/division and differentiation of stem cells is crucial in determining embryonic stem (ES) cell fate.
Shuxian Jiang, Yigong Fu, John Williams, Jodianne Wood, Lakshmipathi Pandarinathan, Shiri Avraham, Alexandros Makriyannis, Shalom Avraham, Hava Karsenty Avraham   +8 more
doaj   +1 more source

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

In silico prediction of novel effective combinational treatment of chronic pain in individual patients: A joint white paper of the H2020 QSPainRelief consortium

British Journal of Pharmacology, EarlyView.
Abstract Opioids are prescribed widely for chronic pain despite well‐recognised risks and variable long‐term benefit, reflecting the lack of effective alternatives for many patients. Combination therapies offer a promising strategy to enhance efficacy whilst reducing side effects.
André Mouraux, Solenn Gousset, Beltrán Alvarez, Monica Baiula, Wouter Bakker, Andrea Bedini, Monir Bertayli, Divakar Budda, Robert Carr, Elisabetta Cuna, Óscar Díaz, Nina Donner, Jesús Giraldo, Geert‐Jan Groeneveld, Berfin Gülave, David Guydan, Hemme Hijma, Rafael Maldonado, Pedro Renault, Carlos Rinaudo, Jeroen Elaissaiss‐Schaap, Athan Spiros, Sara Stoeber, Petri Takkala, Daan van Valkengoed, Coen van Hasselt, Elizabeth (Liesbeth) CM de Lange   +26 more
wiley   +1 more source

3-Hydroxypropane-1,2-Diyl Dipalmitoleate—A Natural Compound with Dual Roles (CB1 Agonist/FAAH1 Blocker) in Inhibiting Ovarian Cancer Cell Line

Pharmaceuticals, 2021
Though it was once known that upregulated Cannabinoid Receptor (CB1) and downregulated Fatty Acid Amide Hydrolase (FAAH1) are associated with tumour aggressiveness and metastasis, it is now clear that upregulated CB1 levels more than a certain point ...
Christina Vijayaraghavan Sathynathan, Lakshmi Sundaram Raman, Sivamurugan Vajiravelu, Thirumal D. Kumar, Thyagarajan Sadras Panchatcharam, Gopinathan Narasimhan, George C. Priya Doss, Mary Elizabeth Gnanambal Krishnan   +7 more
doaj   +1 more source

In vitro determination of the efficacy of illicit synthetic cannabinoids at CB1 receptors

British Journal of Pharmacology, 2019
The morbidity and mortality associated with recreational use of synthetic cannabinoid receptor agonists (SCRAs) may reflect strong activation of CB1 receptors and is a major health concern.
Shivani Sachdev, K. Vemuri, S. Banister, Mitchell Longworth, M. Kassiou, Marina J. Santiago, A. Makriyannis, M. Connor   +7 more
semanticscholar   +1 more source

Neuronal and ion channel mechanisms of noxious heat sensing in mammals: A puzzle of sensory physiology and pharmacology

British Journal of Pharmacology, EarlyView.
Transient receptor potential vanilloid 1 (TRPV1) was the first noxious heat‐sensitive channel discovered. In rodents, its role is robust in the heat response of the cell body of polymodal nociceptors, but surprisingly small in that of the peripheral terminals in the skin.
Gábor Pethő, Peter W. Reeh
wiley   +1 more source

CB1 receptor agonist and heroin, but not cocaine, reinstate cannabinoid‐seeking behaviour in the rat [PDF]

British Journal of Pharmacology, 2004
We recently provided evidence for a functional link between cannabinoid and opioid endogenous systems in relapse to heroin‐seeking behaviour in rats. In the present study, we aimed at investigating whether the previously observed cross‐talk between cannabinoids and opioids could be extended to mechanisms underlying relapse to cannabinoid‐seeking ...
SPANO, MARIA SABRINA, Fattore L, Cossu G, Deiana S, FADDA, PAOLA, FRATTA, WALTER   +5 more
openaire   +3 more sources