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-168734
    CB2 receptor agonist 9
    		Agonist
    CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model.
    CB2 receptor agonist 9
  • HY-125407S
    Palmitoyl serinol-d5
    Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol. 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-d<sub>5</sub>
  • 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-128040
    Virodhamine hydrochloride
    		Antagonist
    Virodhamine (hydrochloride) is a cannabinoid CB1 receptor partial agonist and cannabinoid CB2 receptor full agonist.
    Virodhamine hydrochloride
  • HY-W011040
    LY320135
    		Antagonist
    LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
    LY320135
  • 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-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-178857
    CB1 antagonist 6
    		Antagonist
    CB1 antagonist 6 (Compound 11jE2) is an orally active CB1R antagonist, with an IC50 value of 23 nM. CB1 antagonist 6 significantly reduces food intake and body weight, improves glucose tolerance and insulin resistance, and decreases serum ALT and AST levels in diet-induced obese (DIO) mice, demonstrating hepatoprotective effects. CB1 antagonist 6 can be used for the study of metabolic syndrome (obesity, diabetes).
    CB1 antagonist 6
  • HY-14140
    BPR-890
    		Agonist
    BPR-890 is a potent agonist of CB1. BPR-890 exhibits excellent CB2/1 selectivity and has in vivo efficacy in diet-induced obese mouse model.
    BPR-890
  • HY-B0151S1
    Pregnenolone-13C2,d2
    		99.2%
    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-178943
    Neuroprotective agent 15
    		Agonist
    Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
    Neuroprotective agent 15
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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