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Crystal structures of agonist-bound human cannabinoid receptor CB1
TLDR
The structures reveal important insights into the activation mechanism of CB1 and provide a molecular basis for predicting the binding modes of Δ9-THC, and endogenous and synthetic cannabinoids and should inspire the design of chemically diverse ligands with distinct pharmacological properties.
Cannabinoid receptor stimulation increases motivation for nicotine and nicotine seeking
TLDR
Findings indicate that cannabinoid CB1‐receptor stimulation increases the reinforcing effects of nicotine and precipitates relapse to nicotine‐seeking behaviour in abstinent subjects, and modulating CB1-receptor signalling might have therapeutic value for treating nicotine dependence.
Effects of various cannabinoid ligands on choice behaviour in a rat model of gambling
TLDR
The results suggest that stimulation of cannabinoid receptors could affect gambling choice behaviours differentially in some subgroups of subjects.
Blockade of Nicotine and Cannabinoid Reinforcement and Relapse by a Cannabinoid CB1-Receptor Neutral Antagonist AM4113 and Inverse Agonist Rimonabant in Squirrel Monkeys
TLDR
Both rimonabant and AM4113 reduced cue- induced reinstatement in monkeys trained to self-administer cocaine, suggesting the involvement of a common cannabinoid-mediated mechanism in the cue-induced reinstatement for different drugs of abuse.
Crystal Structure of the Human Cannabinoid Receptor CB 1
Tian Hua1,2, Kiran Vemuri3, Mengchen Pu2, Lu Qu1,2, Gye Won Han4, Yiran Wu1, Suwen Zhao1, Wenqing Shui1, Shanshan Li1, Anisha Korde3, Robert B. Laprairie5, Edward L. Stahl5, Jo-Hao Ho5, Nikolai
The CB1 Neutral Antagonist AM4113 Retains the Therapeutic Efficacy of the Inverse Agonist Rimonabant for Nicotine Dependence and Weight Loss with Better Psychiatric Tolerability
TLDR
The results indicate that AM4113 could be a promising therapeutic option for the prevention of relapse to nicotine-seeking while lacking anxiety/depression-like side effects.
Dual therapy targeting the endocannabinoid system prevents experimental diabetic nephropathy
TLDR
Converging anti-inflammatory mechanisms provide an explanation for this greater efficacy as dual therapy abolished diabetes-induced renal monocyte infiltration and M1/M2 macrophage imbalance in vivo and abrogated the profibrotic effect of M1 Macrophage-conditioned media on cultured mesangial cells.
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