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-15451
    MDA 19
    		Agonist 99.26%
    MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.
    MDA 19
  • HY-100488
    Bay 59-3074
    		Agonist 98.60%
    Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
    Bay 59-3074
  • HY-13288
    Org 27569
    		Modulator 99.40%
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
    Org 27569
  • HY-P1091
    Hemopressin (human, mouse)
    		Antagonist 99.95%
    Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
    Hemopressin (human, mouse)
  • HY-159115
    ART26.12
    		99.57%
    ART26.12 is an orally active FABP5 inhibitor with anti-cannabinoid properties. ART26.12 effectively prevents and alleviates Oxaliplatin (HY-17371)-induced pain through lipid modulation and cannabinoid receptor activation.
    ART26.12
  • HY-116637
    Tetrahydromagnolol
    		Agonist 99.79%
    Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
    Tetrahydromagnolol
  • HY-119104
    AZD1940
    		Agonist 99.58%
    AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
    AZD1940
  • HY-116649
    CB1 antagonist 2
    		Antagonist 99.88%
    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
    CB1 antagonist 2
  • HY-14788
    Drinabant
    		Antagonist ≥99.0%
    Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.
    Drinabant
  • HY-120423
    AM-6538
    		Antagonist 99.85%
    AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability. AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AM-6538
  • HY-12790
    CB1-IN-1
    		Antagonist 99.83%
    CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.
    CB1-IN-1
  • HY-110206
    AM6545
    		Antagonist 98.3%
    AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications.
    AM6545
  • HY-W011051S
    2-Arachidonoylglycerol-d8
    		Agonist ≥98.0%
    2-Arachidonoylglycerol-d8 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
    2-Arachidonoylglycerol-d<sub>8</sub>
  • HY-130311
    2-Linoleoyl glycerol
    		Inhibitor
    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
  • HY-113689
    GAT211
    		Agonist 99.98%
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.
    GAT211
  • HY-N2911
    Auriculasin
    		98.58%
    Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoid receptor type 1 (CB1) with an IC50 value of 8.92 µM.
    Auriculasin
  • HY-14900
    Tedalinab
    		Agonist 99.94%
    Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.
    Tedalinab
  • HY-152581
    CB2R antagonist 3
    		Antagonist 98.08%
    CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.
    CB2R antagonist 3
  • HY-150029
    CB1/2 agonist 3
    		Agonist 99.83%
    CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively.
    CB1/2 agonist 3
  • HY-10013A
    Taranabant racemate
    		Antagonist 99.84%
    Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.
    Taranabant racemate
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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