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:

Cat. No. Product Name Effect Purity
  • HY-15443
    AM251
    		Antagonist 99.25%
    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-W011051
    2-Arachidonoylglycerol
    		Agonist ≥99.0%
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
  • HY-13439
    SR144528
    		Antagonist 99.25%
    SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
  • HY-B0151
    Pregnenolone
    		Inhibitor 99.87%
    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-149993
    hBChE-IN-2
    		Agonist
    hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities.
  • HY-155967
    CB1R/AMPK modulator 1
    		Antagonist
    CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity.
  • HY-155741
    CB2 PET Radioligand 1
    CB2 PET Radioligand 1 (compound [18F]9) is a PET Radioligand targeting to hCB2 (Ki=7.7 nM). CB2 PET Radioligand 1 is prepared with Cu-mediated 18F-fluorination. CB2 PET Radioligand 1 shows high brain uptake in a murine model of neuroinflammation.
  • HY-18697
    JD-5037
    		Antagonist 98.05%
    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
  • 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-110189
    Pregnenolone monosulfate sodium
    		Inhibitor
    Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-W005629
    Leelamine
    		Agonist 98.36%
    Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity.
  • 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-13505
    AM281
    		Antagonist ≥99.0%
    AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.
  • HY-112340
    TM38837
    		Antagonist 99.00%
    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-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-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.
Cannabinoid Receptor Isoform Comparison

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