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-148909
    Isopropyl dodec-11-enylfluorophosphonate
    		Inhibitor
    Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM).
    Isopropyl dodec-11-enylfluorophosphonate
  • HY-121616
    (R)-SLV 319
    		Antagonist
    (R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319
    (R)-SLV 319
  • HY-145196
    RTICBM-189
    		Modulator 99.73%
    RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats.
    RTICBM-189
  • HY-110189S1
    Pregnenolone monosulfate-d4 sodium
    		Inhibitor
    Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
    Pregnenolone monosulfate-d<sub>4</sub> sodium
  • HY-N0919R
    Yangonin (Standard)
    		Inhibitor
    Yangonin (Standard) is the analytical standard of Yangonin. This product is intended for research and analytical applications. Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin (Standard)
  • HY-125407S
    Palmitoyl serinol-d5
    Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. 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[2][3].
    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-113070
    Dihomo-γ-Linolenoyl Ethanolamide
    		Agonist
    Dihomo-γ-Linolenoyl Ethanolamide, an endocannabinoid, is a cannabinoid (CB) receptor agonist with Kis of 857 nM and 598 nM for human recombinant CB1 and CB2 receptors, respectively.
    Dihomo-γ-Linolenoyl Ethanolamide
  • 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-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[1][2][3][4].
    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-124283A
    LEI-101
    		Agonist
    LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
    LEI-101
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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