1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 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:

  • CB1

  • CB2

Cannabinoid Receptor Related Products (64):

Cat. No. Product Name Effect Purity
  • 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-14137
    Rimonabant Hydrochloride
    Antagonist 99.79%
    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-15443
    AM251
    Antagonist 98.82%
    AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM, also acts as a potent GPR55 agonist with an EC50 of 39 nM.
  • HY-18697
    JD-5037
    Antagonist ≥98.0%
    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-120423
    AM-6538
    Antagonist
    AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability.
  • HY-141411A
    (S)-MRI-1867
    Antagonist
    (S)-MRI-1867 is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS (iNOS) antagonist. (S)-MRI-1867 ameliorates obesity-induced chronic kidney disease (CKD).
  • HY-107471
    CB2 receptor agonist 3
    Agonist
    CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.
  • HY-W011051
    2-Arachidonoylglycerol
    Agonist ≥99.0%
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
  • HY-B0151
    Pregnenolone
    Inhibitor ≥98.0%
    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-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-N1415
    β-Caryophyllene
    Agonist
    β-Caryophyllene is a CB2 receptor agonist.
  • 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-B1739
    Pregnenolone monosulfate
    Inhibitor ≥98.0%
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate 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 can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-W008364
    Olivetol
    Inhibitor ≥98.0%
    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-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-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.
  • 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-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.
Isoform Specific Products

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