2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

Related Products

PDF 1.36 MB

Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Cannabinoid Receptor Isoform Specific Products:

Cannabinoid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10575
    MK-5596
    		Agonist
    MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.
    MK-5596
  • HY-178203
    AM12814
    		Agonist
    AM12814 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.
    AM12814
  • HY-178698
    O-1812
    		Ligand
    O-1812 is a selective CB1 ligand. O-1812 is also a very weak AMT inhibitor. O-1812 can be used in the research of chronic pain, migraines, and inflammation.
    O-1812
  • HY-110020
    rel-O-2050
    		Antagonist
    rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1 receptor antagonist. rel-O-2050 also decreases food intake in mice.
    rel-O-2050
  • HY-182697
    RTICBM-74
    		Modulator
    RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder.
    RTICBM-74
  • HY-152251
    CB2R/FAAH modulator-1
    		Agonist 99.14%
    CB2R/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.
    CB2R/FAAH modulator-1
  • HY-148850
    AZD-2207
    		Antagonist
    AZD-2207 is a cannabinoid receptor CB1 antagonist, known for its high lipophilicity. AZD-2207 has good intestinal permeability in the Caco-2 model and can be used in research related to type 2 diabetes and obesity.
    AZD-2207
  • HY-W013788R
    2-Palmitoylglycerol (Standard)
    		Agonist
    2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.
    2-Palmitoylglycerol (Standard)
  • HY-150028
    CB1/2 agonist 2
    		Agonist
    CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity.
    CB1/2 agonist 2
  • HY-B0151S3
    Pregnenolone-d6
    Pregnenolone-d6 (3β-Hydroxy-5-pregnen-20-one-d6) is the deuterium labeled Pregnenolone (HY-B0151) . Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
    Pregnenolone-d<sub>6</sub>
  • HY-147559
    CB1R Allosteric modulator 2
    		Modulator
    CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
    CB1R Allosteric modulator 2
  • HY-144705
    GAT564
    		Modulator
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.
    GAT564
  • HY-163825A
    (E)-RNB-61
    		Agonist
    (E)-RNB-61 is the E configuration of RNB-61 (HY-163825). RNB-61 is an orally active cannabinoid CB2 receptor (CB2R) agonist with a Ki range of 0.13 nM to 1.81 nM. RNB-61 has renal protective and/or anti-fibrotic effects.
    (E)-RNB-61
  • HY-147558
    CB1R Allosteric modulator 1
    		Modulator
    CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
    CB1R Allosteric modulator 1
  • HY-174335
    UVI3502
    		Antagonist
    UVI3502 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).
    UVI3502
  • HY-149933
    AM841
    		Activator
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility.
    AM841
  • HY-157312
    TM38837
    		Antagonist
    TM38837 is an orally active and selective inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 24 nM. TM38837 has higher selectivity for CB1 than for CB2 (IC50: 4500 nM). TM38837 can reduce body weight, improve plasma inflammatory markers and glucose homeostasis.
    TM38837
  • HY-N15177
    Δ9-THCB
    		Agonist
    Δ9-THCB (Δ9-Tetrahydrocannabutol) has a high affinity for human CB1 and CB2 receptors with the Ki values of 15 nM and 51 nM, respectively. Δ9-THCB (Δ9-Tetrahydrocannabutol) has analgesic and anti-inflammatory activities and plays partial agonistic effects on CB1 receptor in mice.
    Δ9-THCB
  • HY-134615
    Mead ethanolamide
    		Agonist
    Mead ethanolamide is an endogenous cannabinoid receptor agonist with Kd values of 753 nM and 1810 nM against CB1 and CB2, respectively.
    Mead ethanolamide
  • HY-103340
    O-2093
    O-2093 is a selective endocannabinoid anandamide (AEA) reuptake inhibitor with IC50 of 17.3 μM.
    O-2093
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.