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-124954
    MN-25
    		Agonist
    MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has Ki of 245 nM and 11 nM for CB1 and CB2. MN-25 has CB2 agonist activity and inhibits TNF-R release in human peripheral blood mononuclear cells in vitro with an IC50 of 33 μM. MN-25 shows efficacy in a mouse acute inflammation model at oral doses up to 50 mg/kg>[1].
    MN-25
  • HY-174846
    TRPM8 antagonist 4 prodrug
    		Agonist
    TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB2R agonist (EC50: 51.2 nM) and a weak TRPM8 antagonist. TRPM8 antagonist 4 prodrug is a prodrug of TRPM8 antagonist 4 (HY-174825). TRPM8 antagonist 4 prodrug exhibits anti-inflammatory and analgesic activities and can be used in the research of inflammation-related pain disorders.
    TRPM8 antagonist 4 prodrug
  • HY-110041
    L-759656
    		Agonist
    L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin (HY-15371)-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.
    L-759656
  • HY-W008364S1
    Olivetol-d9
    Olivetol-d9 is the deuterium labeled Olivetol. 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[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activities.
    Olivetol-d<sub>9</sub>
  • HY-164817
    CB1/2 receptor-1
    		Agonist
    CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.
    CB1/2 receptor-1
  • HY-155741
    CB2 PET Radioligand 1
    CB2 PET Radioligand 1 (compound [18F]9) is a PET Radioligand targeting to hCB2 (Ki=7.7 nM). CB2 PET Radioligand 1 is prepared with Cu-mediated 18F-fluorination. CB2 PET Radioligand 1 shows high brain uptake in a murine model of neuroinflammation.
    CB2 PET Radioligand 1
  • HY-W770198
    2-Linoleoyl glycerol-d5
    2-Linoleoyl glycerol-d5 (2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 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).
    2-Linoleoyl glycerol-d<sub>5</sub>
  • HY-151107
    CBR Agonist-2
    		Agonist
    CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 and a Ki of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.
    CBR Agonist-2
  • HY-121637
    IDFP
    IDFP (iso-Prdodecylfluorophosphonate) is a chemical affinity probe for the cannabinoid CB1 receptor.
    IDFP
  • HY-149645
    CB2 receptor antagonist 2
    		Antagonist
    CB2 receptor antagonist 2 (compound 39) is a potent antagonist of CB2 with an IC50 value of 0.33 μM. CB2 receptor antagonist 2 has strong interactions with L17, W6.48, V6.51, and C7.42.
    CB2 receptor antagonist 2
  • HY-175730
    CB2R ligand-1
    		Ligand
    CB2R ligand-1 (Compound L14) is a selective Cannabinoid type 2 receptor (CB2R) ligand with a with Ki of 0.16  nM for CB2R over CB1R. CB2R ligand-1 as be used as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation and cancer.
    CB2R ligand-1
  • HY-121947
    1'-Naphthoyl-2-methylindole
    1'-Naphthoyl-2-methylindole (Compound 88) is a cannabinoid mimetics and an inhibitor for Win 55212-2, that inhibits 34% of [3H]Win 55212-2 binding to cannabinoid receptors at 3 μM.
    1'-Naphthoyl-2-methylindole
  • HY-153800A
    (R)-Monlunabant
    		Modulator
    (R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease
    (R)-Monlunabant
  • HY-130357
    15(S)-HETE Ethanolamide
    		Agonist
    15(S)-HETE Ethanolamide is a cannabinoid analog the CB1 receptor (Ki of 600 nM).
    15(S)-HETE Ethanolamide
  • HY-155336
    CB2R agonist 2
    		Agonist
    CB2R agonist 2 (compound cis-17-para) is a CB2R agonist.
    CB2R agonist 2
  • HY-171883
    BI-5756
    		Agonist
    BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases.
    BI-5756
  • HY-147532
    CB2R probe 1
    CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells.
    CB2R probe 1
  • HY-115428
    (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide
    		Agonist
    (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM.
    (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide
  • HY-172409
    CB1R antagonist 2
    		Antagonist
    CB1R antagonist 2 (Compound 11g) is the antagonist for cannabinoid receptor 1 (CB1R), that inhibits MAPK/NF-κB signaling pathway and exhibits anti-inflammatory activity. CB1R antagonist 2 inhibits LPS (HY-D1056)-induced IL-6, IL-1β and TNF-α expressions in RAW264.7. CB1R antagonist 2 ameliorates OVA-induced allergic rhinitis in mouse models.
    CB1R antagonist 2
  • HY-P1091A
    Hemopressin(human, mouse) TFA
    		Antagonist
    Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
    Hemopressin(human, mouse) TFA
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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