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

Cannabinoid Receptor

Cannabinoid Receptor

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:

Cat. No. Product Name Effect Purity
  • HY-15443
    AM251
    Antagonist 98.82%
    AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC50 of 39 nM.
  • HY-14137
    Rimonabant Hydrochloride
    Antagonist 99.95%
    Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
  • HY-13291
    WIN 55,212-2 Mesylate
    Agonist 99.59%
    WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
  • HY-18697
    JD-5037
    Antagonist 98.05%
    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
  • HY-13439
    SR144528
    Antagonist 99.86%
    SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
  • HY-103333
    Arvanil
    ≥99.0%
    Arvanil is a ligand for vanilloid receptor 1 (VR1) and cannabinoid 1 (CB1). Arvanil can inhibit spasticity, as a potent neuroprotectant.
  • HY-148176
    ANEB-001
    Inhibitor
    ANEB-001 is an orally active CB1 inhibitor, can be used to research acute cannabinoid intoxication.
  • HY-147707
    CB2 receptor antagonist 1
    Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
  • HY-W011051
    2-Arachidonoylglycerol
    Agonist ≥99.0%
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
  • HY-B0151
    Pregnenolone
    Inhibitor 98.05%
    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.
  • HY-N1415
    β-Caryophyllene
    Agonist 99.12%
    β-Caryophyllene is a CB2 receptor agonist.
  • HY-10013
    Taranabant
    Inhibitor 99.03%
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  • HY-111110
    Olorinab
    Agonist ≥99.0%
    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
  • HY-W008364
    Olivetol
    Inhibitor 99.81%
    Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
  • HY-14167
    GW842166X
    Agonist 99.97%
    GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.
  • HY-13288
    Org 27569
    Modulator 99.40%
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
  • HY-112340
    TM38837
    Antagonist 99.61%
    TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
  • HY-128872
    EHP-101
    Agonist 98.56%
    EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.
  • HY-16642A
    LY2828360
    Agonist 98.91%
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • HY-113204
    N-Oleoyl glycine
    Activator ≥99.0%
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.

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