Expression of GPR55 and either cannabinoid CB1 or CB2 heteroreceptor complexes in the caudate, putamen, and accumbens nuclei of control, parkinsonian, and dyskinetic non-human primates
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DOI: 10.1007/s00429-020-02116-4
Abstract: Endocannabinoids are neuromodulators acting on specific cannabinoid CB1 and CB2 G-protein-coupled receptors (GPCRs), representing potential therapeutic targets for neurodegenerative diseases. Cannabinoids also regulate the activity of GPR55, a recently “deorphanized” GPCR that directly interacts with… read more here.
Keywords: gpr55; control; expression; cb2 ... See more keywords
Alterations in Gene and Protein Expression of Cannabinoid CB2 and GPR55 Receptors in the Dorsolateral Prefrontal Cortex of Suicide Victims
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DOI: 10.1007/s13311-018-0610-y
Abstract: Recent studies point to the cannabinoid CB2 receptors (CB2r) and the non-cannabinoid receptor GPR55 as potential key targets involved in the response to stress, anxiety, and depression. Considering the close relationship between neuropsychiatric disorders and… read more here.
Keywords: protein expression; gpr55; suicide; suicide victims ... See more keywords
Evaluation of 4-oxo-quinoline-based CB2 PET radioligands in R6/2 chorea huntington mouse model and human ALS spinal cord tissue.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.097
Abstract: The cannabinoid receptor 2 (CB2) has been implicated in a series of neurodegenerative disorders and has emerged as an interesting biological target for therapeutic as well as diagnostic purposes. In the present work, we describe… read more here.
Keywords: huntington; als spinal; cb2; human als ... 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.
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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
Dissecting the role of CB1 and CB2 receptors in cannabinoid reward versus aversion using transgenic CB1- and CB2-knockout mice
Sign Up to like & getrecommendations! Published in 2021 at "European Neuropsychopharmacology"
DOI: 10.1016/j.euroneuro.2020.11.019
Abstract: Cannabinoids produce both rewarding and aversive effects in humans and experimental animals. However, the mechanisms underlying these conflicting findings are unclear. Here we examined the potential involvement of CB1 and CB2 receptors in cannabinoid action… read more here.
Keywords: cb2 receptors; mice; cb2; cb1 cb2 ... See more keywords
Pharmacological inhibition of 2-arachidonoilglycerol hydrolysis enhances memory consolidation in rats through CB2 receptor activation and mTOR signaling modulation
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DOI: 10.1016/j.neuropharm.2018.05.030
Abstract: ABSTRACT The endocannabinoid system is a key modulator of memory consolidation for aversive experiences. We recently found that the fatty acid amide hydrolase (FAAH) inhibitor URB597, which increases anandamide levels by inhibiting its hydrolysis, facilitates… read more here.
Keywords: consolidation; cb2; activation; memory consolidation ... See more keywords
The tamoxifen derivative ridaifen‐B is a high affinity selective CB2 receptor inverse agonist exhibiting anti‐inflammatory and anti‐osteoclastogenic effects
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DOI: 10.1016/j.taap.2018.06.009
Abstract: &NA; Selective estrogen receptor modulators (SERMs) target estrogen receptors (ERs) to treat breast cancer and osteoporosis. Several SERMs exhibit anti‐cancer activity not related to ERs. To discover novel anti‐cancer drugs acting via ER‐independent mechanisms, derivatives… read more here.
Keywords: anti inflammatory; inverse agonist; high affinity; affinity ... See more keywords
Identification of Novel CB2 Ligands through Virtual Screening and In Vitro Evaluation
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DOI: 10.1021/acs.jcim.2c01503
Abstract: Cannabinoid receptor type 2 (CB2) is a very promising therapeutic target for a variety of potential indications. However, despite the existence of multiple high affinity CB2 ligands, none have yet been approved as a drug.… read more here.
Keywords: cb2 ligands; virtual screening; novel cb2; cb2 ... See more keywords
Identification and Preclinical Development of a 2,5,6-Trisubstituted Fluorinated Pyridine Derivative as a Radioligand for the Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors.
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DOI: 10.1021/acs.jmedchem.0c00778
Abstract: Despite the broad implications of the cannabinoid type 2 receptor (CB2) in neuroinflammatory processes, a suitable CB2-targeted probe is currently lacking in clinical routine. As part of our medicinal chemistry program, we have recently identified… read more here.
Keywords: cannabinoid type; pyridine; chemistry; cb2 ... See more keywords
Cannabinoid CB2 receptors mediate the anxiolytic-like effects of monoacylglycerol lipase inhibition in a rat model of predator-induced fear
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DOI: 10.1038/s41386-020-0696-x
Abstract: The endocannabinoid system is a key regulator of the response to psychological stress. Inhibitors of monoacylglycerol lipase (MGL), the enzyme that deactivates the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG), exert anxiolytic-like effects in rodent models via 2-AG-dependent activation… read more here.
Keywords: cb2 receptors; induced fear; like effects; cb2 ... See more keywords