Results 1 to 10 of about 454,873 (186)

CB1 Cannabinoid Receptor Signaling and Biased Signaling

Molecules, 2021
The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout the central nervous system that is a promising target for the treatment of various disorders, including anxiety, pain, and neurodegeneration.
Luciana M. Leo, Mary E. Abood
doaj   +2 more sources

Quinazoline-2,4(1H,3H)-dione derivatives as new class of CB1 Agonists: A pharmacophore-based virtual screening workflow and drug discovery. [PDF]

F1000Res
Background The cannabinoid 1 (CB1) receptor is the primary target of Δ9-tetrahydrocannabinol (Δ9-THC), the psychoactive component of cannabis sativa (commonly known as “kif” in Morocco).
El Aissouq A, Stitou M, Enneiymy M, El Rhabori S, Zaitan H, Ouammou A, Khalil F.   +6 more
europepmc   +2 more sources

Targeting the Endocannabinoid CB1 Receptor to Treat Body Weight Disorders: A Preclinical and Clinical Review of the Therapeutic Potential of Past and Present CB1 Drugs

Biomolecules, 2020
Obesity rates are increasing worldwide and there is a need for novel therapeutic treatment options. The endocannabinoid system has been linked to homeostatic processes, including metabolism, food intake, and the regulation of body weight.
Thomas Murphy, Bernard Le Foll
doaj   +2 more sources

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

Br J Pharmacol
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
Solomon ID, Garai S, Thakur GA, Hohmann AG.   +3 more
europepmc   +2 more sources

(+)-Trans-Cannabidiol Is an Agonist at Human CB₂ Receptors. [PDF]

Pharmacol Res Perspect
ABSTRACT (−)‐trans‐Cannabidiol ((−)‐CBD) is a principal phytocannabinoid from Cannabis sativa. (−)‐CBD has complex pharmacology but is a relatively weak inhibitor of CB1 and CB2 receptor signaling. Cannabidiol has two chiral centres and thus four stereoisomers.
Burtchaell PB, Santiago MJ, Wang C, Hagdoost M, Clay EJM, Mohnot D, Connor M.   +6 more
europepmc   +2 more sources

Ontogeny of Endocannabinoid Modulation of Neuromuscular Transmission: Contribution of Postsynaptic Nicotinic Receptors and Butyrylcholinesterase-Sensitive Mechanisms. [PDF]

Cells
Endocannabinoid receptors of the CB1 subtype are the most abundant G-protein-coupled receptors in the central nervous system, where they strongly regulate neurotransmitter release.
Nevsky E, Lenina O, Zueva I, Samigullin D, Malomouzh A, Parpura V, Petrov K.   +6 more
europepmc   +2 more sources

Metabolic Syndrome: From Mechanisms to Therapeutic Interventions. [PDF]

MedComm (2020)
A comprehensive overview of molecular mechanisms delves into the potential disease mechanisms of metabolic syndrome, including complex mechanisms such as insulin resistance, chronic low‐grade inflammation, oxidative stress, and epigenetic modifications, and how these mechanisms contribute to the development of metabolic syndrome. Here, the relationship
Yan M, Xiang Q.
europepmc   +2 more sources

Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain

Bioorganic and Medicinal Chemistry Letters, 2012
Iain Martin, Takao Kiyoi
exaly   +2 more sources

The anti‐nausea effects of CB1 agonists are mediated by an action at the visceral insular cortex

British Journal of Pharmacology, 2012
Linda Parker, C L Limebeer
exaly   +2 more sources

Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro

British Journal of Pharmacology, 2007
A. Thomas, Gemma L. Baillie, A. M. Phillips, R. Razdan, R. A. Ross, R. Pertwee   +5 more
exaly   +2 more sources