The great divide: Separation between in vitro and in vivo effects of PSNCBAM-based CB1 receptor allosteric modulators.
Thomas F. Gamage,Charlotte E. Farquhar,Timothy W. Lefever,Brian F. Thomas,Thuy Nguyen,Yanan Zhang,Jenny L. Wiley +6 more
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TLDR
The investigated the pharmacological effects of PSNCBAM-1 and two structural analogs, RTICBM-15 and -28, as well as pregnenolone, in both signaling and behavioral assays including [35S]GTPγS binding, the cannabinoid tetrad and drug discrimination, and confirmed the established pharmacology ofPSNCB AM and analogs in molecular assays of CB1 receptor function.About:
This article is published in Neuropharmacology.The article was published on 2017-10-01 and is currently open access. It has received 23 citations till now. The article focuses on the topics: Allosteric modulator & Allosteric regulation.read more
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Review of the Endocannabinoid System
Hui-Chen Lu,Ken Mackie +1 more
TL;DR: This review discusses how phytocannabinoids and other exogenous compounds may perturb the ECS, emphasizing examples relevant to psychosis and a description of ECS components and their role in synaptic plasticity and neurodevelopment.
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Overcoming the Psychiatric Side Effects of the Cannabinoid CB1 Receptor Antagonists: Current Approaches for Therapeutics Development.
TL;DR: The progress in the development of therapeutics targeting the cannabinoid receptor 1 in the last two decades is described, including neutral antagonists, peripherally restricted ligands, and allosteric modulators.
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Endocannabinoids in Body Weight Control.
TL;DR: The overall goal is to address the molecular, cellular and pharmacological logic behind central and peripheral eCB-mediated body weight control, and to figure out how these precise mechanistic insights are currently transferred into the development of next generation cannabinoid medicines displaying clearly improved safety profiles, such as significantly reduced side effects.
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Positive allosteric modulation of the type 1 cannabinoid receptor reduces the signs and symptoms of Huntington's disease in the R6/2 mouse model.
Robert B. Laprairie,Amina M. Bagher,Jillian L. Rourke,Adel Zrein,Elizabeth A. Cairns,Melanie E. M. Kelly,Christopher J. Sinal,Pushkar M. Kulkarni,Ganesh A. Thakur,Eileen M. Denovan-Wright +9 more
TL;DR: The data presented here provide the first proof of principle for the use of CB1 PAMs to treat the signs and symptoms of HD.
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The future of type 1 cannabinoid receptor allosteric ligands.
TL;DR: This review of recent progress and future promise of CB1R allosteric modulators is discussed and elucidation of crystal structures ofCB1R and compound design based on structure–activity relationships will advance the field.
References
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Journal ArticleDOI
Isolation and structure of a brain constituent that binds to the cannabinoid receptor
William A. Devane,Lumir Hanus,Aviva Breuer,Roger G. Pertwee,Lesley A. Stevenson,Graeme Griffin,Dan Gibson,Asher Mandelbaum,A. Etinger,Raphael Mechoulam +9 more
TL;DR: In this article, an arachidonylethanthanolamide (anandamide) was identified in a screen for endogenous ligands for the cannabinoid receptor and its structure was determined by mass spectrometry and nuclear magnetic resonance spectroscopy and confirmed by synthesis.
Journal ArticleDOI
Structure of a cannabinoid receptor and functional expression of the cloned cDNA
TL;DR: The cloning and expression of a complementary DNA that encodes a G protein-coupled receptor that is involved in cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana are suggested.
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2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain
Takayuki Sugiura,Sachiko Kondo,Akihiro Sukagawa,Shinji Nakane,A. Shinoda,K. Itoh,Atsushi Yamashita,Keizo Waku +7 more
TL;DR: 2-Arachidonoylglycerol was shown to bind appreciably to the cannabinoid receptor in competitive inhibition experiments and may be an endogenous cannabinoid receptor ligand in the brain.
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Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials
Robin Christensen,Pernelle Kruse Kristensen,Pernelle Kruse Kristensen,Else Marie Bartels,Henning Bliddal,Arne Astrup +5 more
TL;DR: The findings suggest that 20 mg per day rimonabant increases the risk of psychiatric adverse events--ie, depressed mood disorders and anxiety-despite depressed mood being an exclusion criterion in these trials.
Journal Article
Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Christian C. Felder,K. E. Joyce,Eileen M. Briley,Jaleh Mansouri,Ken Mackie,O. Blond,Y. Lai,A. L. Ma,Mitchell R +8 more
TL;DR: Except for its inability to couple to the modulation of Q-type calcium channels or inwardly rectifying potassium channels, the CB1 and CB2 receptors display similar pharmacological and biochemical properties.