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 Related Products (168):

Cat. No. Product Name Effect Purity
  • HY-18697
    JD-5037 Antagonist
    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
  • 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[1][2][3].
  • 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
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
  • 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[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
  • HY-116380
    CB2 receptor antagonist 5
    CB2 receptor antagonist 5 (compound 4A) is a ligand of CB2 receptor with antagonist effect[1].
  • HY-130311
    2-Linoleoyl glycerol Inhibitor
    2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG)[1][2].
  • HY-163394
    CB2 receptor agonist 6 Agonist
    CB2 receptor agonist 6 (compound 70) is an agonist of CB2R, with EC50 of 162 nM. The IC50 values of CB2 receptor agonist 6 are 4.83 μM for CB1R and 0.88 μM for CB2R. CB2 receptor agonist 6 is a neuroprotective agent that can be used for the reseach of neurological disease[1].
  • HY-110179
    PSNCBAM-1 Antagonist 99.48%
    PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity[1].
  • 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-148909
    Isopropyl dodec-11-enylfluorophosphonate Inhibitor
    Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM)[1].
  • 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-121616
    (R)-SLV 319 Antagonist
    (R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319[1]
  • HY-145196
    RTICBM-189 Modulator 99.73%
    RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats[1].
  • HY-14791A
    (±)-Ibipinabant Antagonist 99.90%
    (±)-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-110189S1
    Pregnenolone monosulfate-d4 sodium Inhibitor
    Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. 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[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
  • HY-125407S
    Palmitoyl serinol-d5
    Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. 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[2][3].
  • HY-161311
    AChE/BChE-IN-18 Antagonist
    AChE/BChE-IN-18 (Compound 4g) is a dual inhibitor of AChE/BChE , with a IC50 value of 0.315 μM for AchE. AChE/BChE-IN-18 is also a CB2R antagonist with a Ki value of 31 nM. AChE/BChE-IN-18 has neuroprotective activity[1].
  • HY-128040
    Virodhamine hydrochloride Antagonist
    Virodhamine (hydrochloride) is a cannabinoid CB1 receptor partial agonist and cannabinoid CB2 receptor full agonist[1].
  • HY-113689
    GAT211 Agonist
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research[1].