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:

Cannabinoid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0151S1
    Pregnenolone-13C2,d2
    Pregnenolone-13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone 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[1][2][3][4].
    Pregnenolone-<sup>13</sup>C<sub>2</sub>,d<sub>2</sub>
  • HY-139230
    OLHHA
    		Antagonist
    OLHHA is a dual CB1 receptor antagonist and PPARα agonist. OLHHA also is a alcohol intake inhibitor with an EC50 value of 0.2 mg/kg. OLHHA reduces both hepatic lipid accumulation and circulating triglyceride levels. OLHHA shows anti-steatotic activity and has the potential for the research of non-alcoholic fatty liver disease (NAFLD).
    OLHHA
  • HY-113885
    MDA77
    		Agonist
    MDA77 is a CB2 inverse agonist with an EC50 of 5.82 nM, showing selectivity for human CB2 and no activity on CB1.
    MDA77
  • HY-150057
    CB1R Allosteric modulator 4
    		Modulator
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.
    CB1R Allosteric modulator 4
  • 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.
    hBChE-IN-2
  • HY-119744
    BAY 38-7271
    		Agonist
    BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
    BAY 38-7271
  • HY-100328
    CB2R-IN-1
    		Inhibitor
    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
    CB2R-IN-1
  • HY-150056
    CB1R Allosteric modulator 3
    		Modulator 98.05%
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.
    CB1R Allosteric modulator 3
  • HY-118245
    APP-FUBINACA
    		Agonist
    APP-FUBINACA is a cannabinoid receptor agonist and a derivative of phenylalaninamide-based indazole-3-carboxamide. APP-FUBINACA exhibits neurostimulatory effects.
    APP-FUBINACA
  • HY-149644
    CB2R agonist 3
    		Agonist
    CB2R agonist 3 is an agonist of cannabinoid receptor 2 (CB2R), with EC50 of 0.37μM that plays an important role in immune system.
    CB2R agonist 3
  • HY-W751734
    HU 433
    		Agonist
    HU 433 is a synthetic cannabinoid CB2 receptor agonist and is the enantiomer of HU 308 (HY-161510). HU 433 exerts its anti-inflammatory and neuroprotective effects by binding to CB2 receptors. HU 433 can be used in the study of neuroinflammation and retinal diseases.
    HU 433
  • HY-122281
    JTE 7-31
    		Agonist
    JTE 7-31 selectively acts on peripheral cannabinoid receptors, minimizing central nervous system side effects. They exhibit potent immunomodulatory, anti-inflammatory and anti-allergic properties, as well as inhibitory effects on nephritis.
    JTE 7-31
  • HY-125743
    S-1 Methanandamide
    		Agonist 98.00%
    S-1 Methanandamide ((S)-Methanandamide), an Anandamide analog, is a CB1 receptor ligand with a Ki of 173 nM. S-1 Methanandamide inhibits electrically-evoked twitch response in mouse vas deferens with an IC50 value of 230 nM.
    S-1 Methanandamide
  • HY-116380
    CB2 receptor antagonist 5
    CB2 receptor antagonist 5 (compound 4A) is a ligand of CB2 receptor with antagonist effect.
    CB2 receptor antagonist 5
  • HY-14160
    CB2 receptor agonist 7
    		Agonist
    CB2 receptor agonist 7 (Compound 5B) is a cannabinoid 2 (CB2) receptor agonist with blood-brain barrier permeability.
    CB2 receptor agonist 7
  • HY-14136S
    Rimonabant-d10
    		Antagonist
    Rimonabant-d10 is deuterium labeled Rimonabant. 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-d<sub>10</sub>
  • HY-164913
    PSB-SB-1203
    		Modulator
    PSB-SB-1203 (Compound 25b) is a dual CB1/CB2 ligand that blocks CB1 but activates CB2 receptors (CB1 Ki 0.244 μM; CB2 Ki 0.210 μM, EC50 0.054 μM). PSB-SB-1203 is promising for research of obesity and cancers.
    PSB-SB-1203
  • HY-100778
    SMM-189
    		Agonist
    SMM-189 is  a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research.
    SMM-189
  • 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.
    CB1R/AMPK modulator 1
  • HY-173083
    MDA7
    		Agonist
    MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.
    MDA7
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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