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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CB2R agonist 1
0 ImagesCat. No.: HY-152576CAS No.: 1817633-49-0CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role.
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AM12814
0 ImagesCat. No.: HY-178203CAS No.: 3054511-18-8AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.
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CB2R/FAAH modulator-1
0 ImagesCB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production.
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CB1/2 agonist 2
0 ImagesCat. No.: HY-150028CAS No.: 2772379-97-0
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(E)-RNB-61
0 ImagesCat. No.: HY-163825ACAS No.: 1217403-51-4
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UVI3502
0 ImagesCat. No.: HY-174335UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).
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Δ9-THCB
0 ImagesCat. No.: HY-N15177CAS No.: 60008-00-6Synonyms: Δ9-Tetrahydrocannabutol
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Mead ethanolamide
0 ImagesCat. No.: HY-134615CAS No.: 169232-04-6Mead ethanolamide is an endogenous cannabinoid receptor agonist with Kd values of 753 nM and 1810 nM against CB1 and CB2, respectively.
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PM226
0 ImagesCat. No.: HY-136238CAS No.: 1949726-13-9PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
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CB2R antagonist 4
0 ImagesCat. No.: HY-175784CAS No.: 1341021-90-6CB2R antagonist 4 is a selective CB2R antagonist/inverse agonist with a pKi of 6.54. CB2R antagonist 4 shows a ≥11-fold selectivity towards CB2R over CB1R and can be utilized in neurological research.
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CBR Agonist-1
0 ImagesCat. No.: HY-151105CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases.
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AB-FUBICA
0 ImagesCat. No.: HY-117403CAS No.: 1801338-22-6AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC50 values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms.
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9β,10β-epoxy Hexahydrocannabinol
0 ImagesCat. No.: HY-179436CAS No.: 1781270-07-2Synonyms: 9β,10β-EHHC; 9β,10β-epoxy HHC9β,10β-epoxy Hexahydrocannabinol is a cannabinoid receptor 1 (CB1) and CB2 receptor ligand with a binding affinity of 224 nM for CB1 and 335 nM for CB2. 9β,10β-epoxy Hexahydrocannabinol reduces locomotor activity, induces catalepsy, lowers body temperature, and produces antinociceptive effects in mice. 9β,10β-epoxy Hexahydrocannabinol can be used for the study of nervous system diseases.
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AM11638
0 ImagesCat. No.: HY-176544CAS No.: 3054510-97-0
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CB2R agonist 4
0 ImagesCat. No.: HY-175481CAS No.: 182496-82-8CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. CB2R agonist 4 can induce cell apoptosis, ROS production and protein misfolding. CB2R agonist 4 shows cytotoxicity to a panel of tumor cell lines. CB2R agonist 4 can be used for the research of cancer.
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GW 833972A (Standard)
0 ImagesCat. No.: HY-101765RCAS No.: 1092502-33-4GW 833972A (Standard) is the analytical standard of GW 833972A (HY-101765). This product is intended for research and analytical applications. GW 833972A is a selective CB₂ receptor agonist with pEC₅₀ of the human CB₂ receptor for GW 833972A of 7.3, and its selectivity for the CB₂ receptor is approximately 1000 times higher than that for the CB₁ receptor. GW 833972A inhibits induced neuronal depolarization and suppresses coughing caused by citric acid in guinea pig models. GW 833972A can be used for the study of chronic cough.
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PF-03550096
0 ImagesCat. No.: HY-129787CAS No.: 910376-39-5PF-03550096 is an orally active synthetic cannabinoid (CB) that selectively targets peripheral CB2 receptors with a Ki value of 7.9 nM. PF-03550096 has analgesic activity.
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O-1663
0 ImagesCat. No.: HY-114802CAS No.: 468083-84-3O-1663 is a full agonist of cannabinoid receptor 2 (CB2 receptor). O-1663 stimulates the production of ROS, downregulates Id1, and induces autophagy and apoptosis in breast cancer cells. O-1663 inhibits the proliferation, invasion and metastasis of breast cancer cells. O-1663 prolongs the survival of models with advanced metastatic breast cancer. O-1663 can be used for the research of metastatic breast cancer.
