Design, synthesis, and structure–activity relationships of diindolylmethane derivatives as cannabinoid CB2 receptor agonists
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200493
Abstract: 3,3′‐Diindolylmethane (DIM), a natural product‐derived compound formed upon ingestion of cruciferous vegetables, was recently described to act as a partial agonist of the anti‐inflammatory cannabinoid (CB) receptor subtype CB2. In the present study, we synthesized… read more here.
Keywords: receptor agonists; design synthesis; cb2 receptor; efficacy ... See more keywords
Strategies to develop selective CB2 receptor agonists from indole carboxamide synthetic cannabinoids.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.07.036
Abstract: Activation of the CB2 receptor is an attractive therapeutic strategy for the treatment of a wide range of inflammatory diseases. However, receptor subtype selectivity is necessary in order to circumvent the psychoactive effects associated with… read more here.
Keywords: selective cb2; synthetic cannabinoids; cb2 receptor; develop selective ... See more keywords
Identification and biochemical analyses of selective CB2 agonists.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2019.03.054
Abstract: Cannabinoid CB1 and CB2 receptors are activated by Δ9-tetrahydrocannabinol, a psychoactive component of marijuana. The cannabinoid CB1 receptor is primarily located in the brain and is responsible for the psychoactive side effects, whereas the cannabinoid… read more here.
Keywords: cannabinoid cb1; cb2 receptor; cannabinoid cb2; cb2 ... See more keywords
Activation of cannabinoid type 2 receptor protects skeletal muscle from ischemia-reperfusion injury partly via Nrf2 signaling.
Sign Up to like & getrecommendations! Published in 2019 at "Life sciences"
DOI: 10.1016/j.lfs.2019.05.056
Abstract: AIMS Cannabinoid type 2 (CB2) receptor activation has been shown to attenuate IRI in various organs. NF-E2-related factor (Nrf2) is an anti-oxidative factor that plays multiple roles in regulating cellular redox homeostasis and modulating cell… read more here.
Keywords: skeletal muscle; receptor activation; cb2 receptor; activation ... See more keywords
A Single Point Mutation Blocks the Entrance of Ligands to the Cannabinoid CB2 Receptor via the Lipid Bilayer
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.2c00865
Abstract: Molecular dynamic (MD) simulations have become a common tool to study the pathway of ligand entry to the orthosteric binding site of G protein-coupled receptors. Here, we have combined MD simulations and site-directed mutagenesis to… read more here.
Keywords: cannabinoid cb2; cb2 receptor; mutation blocks; receptor ... See more keywords
Design of Negative and Positive Allosteric Modulators of the Cannabinoid CB2 Receptor Derived from the Natural Product Cannabidiol.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00561
Abstract: Cannabidiol (CBD), the second most abundant of the active compounds found in the Cannabis sativa plant, is of increasing interest because it is approved for human use and is neither euphorizing nor addictive. Here, we… read more here.
Keywords: design negative; cb2 receptor; cannabinoid cb2; receptor ... See more keywords
Novel Machaeriol Analogues as Modulators of Cannabinoid Receptors: Structure–Activity Relationships of (+)-Hexahydrocannabinoids and Their Isoform Selectivities
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DOI: 10.1021/acsomega.1c02413
Abstract: Machaeriols are an important class of compounds that structurally resemble tetrahydrocannabinol (Δ9-THC), with the major differences being inverted stereochemistry at the ring junction as [6aR, 10aR] and an additional stereocenter at the C9 position of… read more here.
Keywords: activity relationships; cb2 receptor; cannabinoid receptors; structure activity ... See more keywords
Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation.
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DOI: 10.1039/c9md00173e
Abstract: The CB2 receptor plays a crucial role in analgesia and anti-inflammation. To develop novel CB2 agonists with high efficacy and selectivity, a series of indole derivatives with N-ethyl morpholine moieties (compounds 1-56) were designed, synthesized… read more here.
Keywords: cb2 receptor; ethyl morpholine; compound; receptor ... See more keywords
P4140Myeloid but not endothelial expression of the CB2 receptor promotes atherogenesis in the context of elevated levels of the endocannabinoid 2-arachidonoylglycerol
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DOI: 10.1093/eurheartj/ehz745.0712
Abstract: The endocannabinoid 2-arachidonoylglycerol (2-AG) is an inflammatory mediator and ligand to the cannabinoid receptors CB1 and CB2, which are expressed on myeloid and endothelial cells. 2-AG has recently been described to promote atherogenesis in ApoE-deficient… read more here.
Keywords: elevated levels; cb2 receptor; expression; mice ... See more keywords
Anandamide Hydrolysis Inhibition Reverses the Long-Term Behavioral and Gene Expression Alterations Induced by MK-801 in Male Rats: Differential CB1 and CB2 Receptor-Mediated Effects.
Sign Up to like & getrecommendations! Published in 2022 at "Schizophrenia bulletin"
DOI: 10.1093/schbul/sbab153
Abstract: NMDA receptor blockade in rodents is commonly used to induce schizophrenia-like behavioral abnormalities, including cognitive deficits and social dysfunction. Aberrant glutamate and GABA transmission, particularly in adolescence, is implicated in these behavioral abnormalities. The endocannabinoid… read more here.
Keywords: cb2 receptor; cb1 cb2; expression; glutamate gaba ... See more keywords
An overview of the cannabinoid type 2 receptor system and its therapeutic potential
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DOI: 10.1097/aco.0000000000000616
Abstract: Purpose of review This narrative review summarizes recent insights into the role of the cannabinoid type 2 (CB2) receptor as potential therapeutic target in neuropathic pain and neurodegenerative conditions. Recent findings The cannabinoid system continues… read more here.
Keywords: receptor; cannabinoid type; cb2 receptor;