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-125972
    zr17-2
    		Modulator 98.01%
    zr17-2 is a potent cannabinoid CB1 receptor modulator. zr17-2 reduces oxidative stress-induced retinal cell death.
    zr17-2
  • HY-14788
    Drinabant
    		Antagonist ≥99.0%
    Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.
    Drinabant
  • HY-120423
    AM-6538
    		Antagonist 99.85%
    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. AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AM-6538
  • HY-145604
    Vicasinabin
    		Agonist 98.37%
    Vicasinabin (RG7774) is an orally active, selective, and full CB2R agonist, with EC50 values of 2.81 nM and 2.60 nM for human CB2R and mouse CB2R, respectively. Vicasinabin inhibits inflammation, reduces leukocyte adhesion and decreases vascular permeability by selectively activating CB2R. Vicasinabin can be used in the researches for diabetic retinopathy, uveitis and laser-induced choroidal neovascularization.
    Vicasinabin
  • HY-152581
    CB2R antagonist 3
    		Antagonist 98.08%
    CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.
    CB2R antagonist 3
  • HY-101765
    GW 833972A
    		Agonist 99.91%
    GW 833972A is a selective CB2 receptor agonist. GW 833972A inhibits induced nerve depolarization and citric acid-induced cough in animal models.
    GW 833972A
  • HY-125407
    Palmitoyl serinol
    		99.89%
    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.
    Palmitoyl serinol
  • HY-110018
    N-Arachidonyldopamine
    		Agonist 98.36%
    N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM.
    N-Arachidonyldopamine
  • HY-141411A
    Zevaquenabant
    		Antagonist 99.64%
    Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD).
    Zevaquenabant
  • HY-N2911
    Auriculasin
    		Inhibitor 98.58%
    Auriculasin is an anticancer agent that inhibits VEGFR2, PI3K/AKT/mTOR, MAPK. Auriculasin can inhibit cell proliferation, induce cell apoptosis, and inhibit angiogenesis, and promotes mitochondrial oxidative stress and ferroptosis. Auriculasin is also active at the cannabinoid receptor CB1 with an IC50 of 8.92 μM. Auriculasin can be used in cancer research, especially related diseases such as prostate cancer and non-small cell lung cancer, as well as research on the development of anti-angiogenic drugs.
    Auriculasin
  • HY-103333
    Arvanil
    		≥99.0%
    Arvanil is a ligand for vanilloid receptor 1 (VR1) and cannabinoid 1 (CB1). Arvanil can inhibit spasticity, as a potent neuroprotectant.
    Arvanil
  • HY-118140
    ZCZ011
    		Modulator 99.43%
    ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain.
    ZCZ011
  • HY-101389
    (R)-Methanandamide
    		Agonist
    (R)-Methanandamide (AM-356), an analog of the endocannabinoid ligand Anandamide, is a potent CB1 agonist with a Ki of 20 nM. (R)-Methanandamide also activates vanilloid (TRPV1) receptors.
    (R)-Methanandamide
  • HY-12790
    CB1-IN-1
    		Antagonist 99.83%
    CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.
    CB1-IN-1
  • HY-121827
    LH21
    		Antagonist 99.83%
    LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats. , and displays efficacy as a feeding inhibitor.
    LH21
  • HY-14791
    Ibipinabant
    		Antagonist 99.90%
    Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic.
    Ibipinabant
  • HY-121541
    CB-25
    		99.02%
    CB-25 is a ligand of CB1 cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin (HY-15371)-induced cAMP formation in cancer cells but not hCB1-CHO cells.
    CB-25
  • HY-10863S
    Anandamide-d8
    		Agonist 99.90%
    Anandamide-d8 is a deuterated labeled Anandamide. Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.
    Anandamide-d<sub>8</sub>
  • HY-12761
    A-836339
    		Agonist 99.84%
    A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc.
    A-836339
  • HY-148176
    ANEB-001
    		Inhibitor
    ANEB-001 is an orally active CB1 inhibitor, can be used to research acute cannabinoid intoxication.
    ANEB-001
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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