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-167865
    O-1269
    		Agonist
    O-1269 is a partial agonist of cannabinoid receptor 1 (CB1R) with a Ki of 32 nM. O-1269 shows analgesic effects.
    O-1269
  • HY-133533
    O-2050
    		Antagonist
    O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice.
    O-2050
  • HY-121545
    CB-52
    		Antagonist
    CB-52 is the ligand and neutral antagonist of CB2 cannabinoid receptor.
    CB-52
  • HY-174825
    TRPM8 antagonist 4
    		Agonist
    TRPM8 antagonist 4 is a CB2R partial agonist (EC50=54.2 nM, Ki=3.2 μM) and TRPM8 antagonists (IC50=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β.
    TRPM8 antagonist 4
  • HY-168338
    CB2 receptor agonist 8
    		Agonist
    CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87.
    CB2 receptor agonist 8
  • HY-169038
    11(Z),14(Z)-Eicosadienoic acid ethanolamide
    		Inhibitor
    11(Z),14(Z)-Eicosadienoic acid ethanolamide (Compound 3) is an ethanolamide-conjugated form of 11(Z),14(Z)-Eicosadienoic acid (HY-149589). 11(Z),14(Z)-Eicosadienoic acid ethanolamide inhibits the inactivating transport of an endogenous cannabinoid substance with an IC50 value of 10.6 μM. 11(Z),14(Z)-Eicosadienoic acid ethanolamide can be used for research of neuropsychiatric conditions.
    11(Z),14(Z)-Eicosadienoic acid ethanolamide
  • HY-168997
    CB1R agonist 1
    		Agonist
    CB1R agonist 1 (Compound '1350') is a potent full agonist of the cannabinoid-1 receptor (CB1R), with a Ki value of 0.95 nM. CB1R agonist 1 exhibits significant pain-reducing effects in multiple pain models, including acute heat pain, inflammatory pain, and neuropathic pain.
    CB1R agonist 1
  • HY-155481
    CB2 receptor antagonist 3
    		Chemical
    CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes.
    CB2 receptor antagonist 3
  • HY-103336
    Tocrifluor 1117
    		Antagonist
    Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm).
    Tocrifluor 1117
  • 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.
    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
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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