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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    AM251
  • 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).
    Rimonabant Hydrochloride
  • HY-W011051
    2-Arachidonoylglycerol
    Agonist ≥99.0%
    2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
    2-Arachidonoylglycerol
  • 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.
    Pregnenolone
  • HY-18697
    JD-5037
    Antagonist 98.05%
    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
    JD-5037
  • HY-110036A
    GW405833 hydrochloride
    Agonist 99.59%
    GW405833 hydrochloride is a potent and selective cannabinoid-2 (CB2) receptor agonist (EC50 = 0.65 nM; maximum inhibition = 44.6%). GW405833 hydrochloride produces potent antihyperalgesic effects in several rodent models of pain.
    GW405833 hydrochloride
  • 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).
    Isopropyl dodec-11-enylfluorophosphonate
  • 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.
    AChE/BChE-IN-18
  • HY-N1415
    β-Caryophyllene
    Agonist 99.12%
    β-Caryophyllene is a CB2 receptor agonist.
    β-Caryophyllene
  • HY-13439
    SR144528
    Antagonist 99.25%
    SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
    SR144528
  • HY-10013
    Taranabant
    Inhibitor 99.06%
    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.
    Taranabant
  • HY-14136
    Rimonabant
    Antagonist 99.41%
    Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant
  • 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.
    Pregnenolone monosulfate sodium
  • HY-111110
    Olorinab
    Agonist 99.29%
    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.
    Olorinab
  • 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.
    Olivetol
  • 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.
    Leelamine
  • HY-N0919
    Yangonin
    Inhibitor 99.79%
    Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin
  • HY-16642A
    LY2828360
    Agonist 98.41%
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
    LY2828360
  • HY-B1161A
    S-Methoprene
    Antagonist
    S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [3H]CP-55940 to the CB1 receptor (IC50: 19.31 μM).
    S-Methoprene
  • 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.
    AM281

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