CB2
Cannabinoid receptor CB2 (CB2R) is a cannabinoid G protein-coupled receptor originally characterized as a peripheral receptor expressed in macrophages and immune tissues[1][2]. Mechanistically, CB2R couples through Gi/o proteins, inhibits adenylyl cyclase, and activates MAPK signaling, linking cannabinoid receptor signaling to immune-cell regulation[3]. In inflammatory biology, CB2R modulates immune-cell functions in cell systems and animal models, and CB2-deficient mice show exacerbated inflammatory phenotypes[2]. In neuroinflammation, CB2R activity is especially relevant in macrophage-lineage cells and CNS microglia, connecting peripheral immune regulation with central immune responses[4]. Compared with CB1, CB2 is distinguished by immune-enriched distribution, while CB1 is found predominantly in neuronal tissues and also couples to ion-channel signaling[5]. For experimental applications, CB2-selective agonists such as HU-308 bind CB2 efficiently, inhibit forskolin-stimulated cyclic AMP production in CB2-transfected cells, and support receptor-selective studies of inflammation and peripheral analgesia[6].- CB2R links cannabinoid receptor signaling with immune modulation, inflammation models, and neuroimmune research design[2][4]. - CB2 differs from CB1 mainly by immune distribution, not by complete separation of signaling pathways[5]. - HU-308 supports CB2-selective pharmacology studies in inflammation, peripheral analgesia, and cAMP assays[6].
References:
- [1]. Munro S, et al. Molecular characterization of a peripheral receptor for cannabinoids. Nature. 1993 Sep 2;365(6441):61-5. [Content Brief]
- [2]. Turcotte C, et al. The CB2 receptor and its role as a regulator of inflammation. Cell Mol Life Sci. 2016 Dec;73(23):4449-4470. [Content Brief]
- [3]. Howlett AC. Cannabinoid receptor signaling. Handb Exp Pharmacol. 2005;(168):53-79. [Content Brief]
- [4]. Cabral GA, et al. Emerging role of the cannabinoid receptor CB2 in immune regulation: therapeutic prospects for neuroinflammation. Expert Rev Mol Med. 2009 Jan 20;11:e3. [Content Brief]
- [5]. Howlett AC, et al. International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev. 2002 Jun;54(2):161-202. [Content Brief]
- [6]. Hanus L, et al. HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor. Proc Natl Acad Sci U S A. 1999 Dec 7;96(25):14228-33. [Content Brief]
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CB2 Related Products (82)
Related Products (82)
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AZD1940
0 ImagesAZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
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JTE-907
0 ImagesJTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.
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L759633
0 ImagesL759633 is a potent and selective agonist of cannabinoid receptor (CB2) receptor, with Kis of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production.
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Bay 59-3074
0 ImagesBay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
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Noladin ether
0 ImagesCat. No.: HY-110014CAS No.: 222723-55-9Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.
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CB2 modulator 1
0 ImagesCB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia.
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Tedalinab
0 ImagesSynonyms: GRC-10693Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.
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CB2R/FAAH modulator-3
0 ImagesCB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
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Vicasinabin
0 ImagesSynonyms: RG7774Vicasinabin (RG7774) is an orally active, selective, and full CB2R agonist, with EC50 values of 2.81 nM and 2.60 nM for human CB2R and mouse CB2R, respectively. Vicasinabin inhibits inflammation, reduces leukocyte adhesion and decreases vascular permeability by selectively activating CB2R. Vicasinabin can be used in the researches for diabetic retinopathy, uveitis and laser-induced choroidal neovascularization.
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CB2R antagonist 3
0 ImagesCat. No.: HY-152581Purity: 98.08%CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.
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CB2 receptor agonist 9
0 ImagesCat. No.: HY-168734CAS No.: 2374894-21-8
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(±)5(6)-EET Ethanolamide
0 ImagesCat. No.: HY-172568(±)5(6)-EET Ethanolamide is a metabolite of Anandamide (HY-10863) generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.
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LY320135
0 ImagesCat. No.: HY-W011040CAS No.: 176977-56-3LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
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O-2050
0 ImagesCat. No.: HY-133533CAS No.: 1883545-42-3O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice.
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TRPM8 antagonist 4
0 ImagesCat. No.: HY-174825CAS No.: 3107363-68-5TRPM8 antagonist 4 is a CB2R partial agonist (EC50=54.2 nM, Ki=3.2 μM) and TRPM8 antagonists (IC50=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β.
