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 (51):

Cat. No. Product Name Effect Purity
  • HY-13291
    WIN 55,212-2 Mesylate Agonist 99.01%
    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 hHydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
  • HY-13439
    SR144528 Antagonist 99.86%
    SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
  • HY-15443
    AM251 Antagonist 99.92%
    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 98.77%
    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
  • HY-15421
    6-Iodopravadoline Antagonist 99.35%
    6-Iodopravadoline (AM630) is a selective CB2 antagonist with Ki of 31.2 nM, and displays 165-fold selectivity over CB1 receptors.
  • HY-101995
    Ridaifen-B Antagonist
    Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen (HY-13757A) derivative. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects.
  • HY-W011040
    LY320135 Antagonist
    LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
  • HY-10013
    Taranabant Inhibitor 99.28%
    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-W011051
    2-Arachidonoylglycerol Agonist >99.0%
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
  • HY-10863
    Anandamide Activator >99.0%
    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  • HY-N1415
    β-Caryophyllene Agonist
    β-Caryophyllene is a CB2 receptor agonist.
  • 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.
  • HY-16642A
    LY2828360 Agonist 98.99%
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • 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-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-100488
    Bay 59-3074 Agonist 98.85%
    Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
  • HY-14791A
    (±)-Ibipinabant Antagonist 99.93%
    (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
  • HY-10871
    Otenabant Antagonist 99.65%
    Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
  • 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.
Isoform Specific Products

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