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

Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

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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-125407
    Palmitoyl serinol
    Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin.
    Palmitoyl serinol
  • HY-12095
    CB1 inverse agonist 2
    		Agonist
    CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model.
    CB1 inverse agonist 2
  • HY-150030
    CB1/2 agonist 4
    		Agonist
    CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively.
    CB1/2 agonist 4
  • HY-110048
    O-2545 hydrochloride
    		Activator
    O-2545 hydrochloride is a highly potent, water-soluble CB1/CB2 receptor agonist (with Ki values of 1.5 and 0.32 nM for CB1 and CB2 respectively), can be used for epilepsy, pain, multiple sclerosis research.
    O-2545 hydrochloride
  • HY-120300
    UCM710
    		Inhibitor
    UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase.
    UCM710
  • HY-107019
    Surinabant
    		Antagonist
    Surinabant (SR 147778) is an orally active, selective cannabinoid receptor type 1 CB1R antagonist. Surinabant is used in studies of obesity and alcoholism.
    Surinabant
  • 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-152251
    CB2R/FAAH modulator-1
    		Agonist
    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-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-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-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-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
  • HY-W337358
    N-(3-Hydroxyphenyl)-arachidonoyl amide
    		Inhibitor
    N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC50 of 21.3 μM.
    N-(3-Hydroxyphenyl)-arachidonoyl amide
  • HY-122109A
    Levonantradol hydrochloride
    		Agonist
    Levonantradol (l-Nantradol) hydrochloride is an analog of delta (9)-tetrahydrocannabinol. Levonantradol acting as a potent anti-analgesic agent.
    Levonantradol hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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