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-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-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-125743
    S-1 Methanandamide
    		Agonist ≥98.0%
    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-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-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-125111
    PSB-SB-487
    		Modulator 99.36%
    PSB-SB-487 is a potent GPR55 antagonist and CB2 agonist with an IC50 value of 0.113 µM for GPR55, and a Ki value of 0.292 µM for human CB2. PSB-SB-487 can be used for researching diabetes, Parkinson’s disease, neuropathic pain, and cancer.
    PSB-SB-487
  • 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-B0151S
    Pregnenolone-d4
    		Inhibitor
    Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) 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[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
    Pregnenolone-d<sub>4</sub>
  • 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-W008364R
    Olivetol (Standard)
    		Inhibitor
    Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. 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. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
    Olivetol (Standard)
  • 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-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-153800A
    (R)-Monlunabant
    		Modulator
    (R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease
    (R)-Monlunabant
  • HY-126161
    Nonabine
    		Activator
    Nonabine (BRL-4664), a cannabinoid, is a antiemetic agent. Nonabine activates CB1 receptor in the brainstem and enteric nervous system.
    Nonabine
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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