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-147559
    CB1R Allosteric modulator 2
    		Modulator
    CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
    CB1R Allosteric modulator 2
  • HY-144705
    GAT564
    		Modulator
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.
    GAT564
  • HY-147558
    CB1R Allosteric modulator 1
    		Modulator
    CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
    CB1R Allosteric modulator 1
  • HY-174335
    UVI3502
    		Antagonist
    UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).
    UVI3502
  • HY-149933
    AM841
    		Activator
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility.
    AM841
  • HY-N15177
    Δ9-THCB
    		Agonist
    Δ9-THCB (Δ9-Tetrahydrocannabutol) has a high affinity for human CB1 and CB2 receptors with the Ki values of 15 nM and 51 nM, respectively. Δ9-THCB (Δ9-Tetrahydrocannabutol) has analgesic and anti-inflammatory activities and plays partial agonistic effects on CB1 receptor in mice.
    Δ9-THCB
  • HY-134615
    Mead ethanolamide
    		Agonist
    Mead ethanolamide is an endogenous cannabinoid receptor agonist with Kd values of 753 nM and 1810 nM against CB1 and CB2, respectively.
    Mead ethanolamide
  • HY-103340
    O-2093
    O-2093 is a selective endocannabinoid anandamide (AEA) reuptake inhibitor with IC50 of 17.3 μM.
    O-2093
  • HY-W337358
    N-(3-Hydroxyphenyl)-arachidonoyl amide
    		Inhibitor
    N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC50 of 21.3 μM.
    N-(3-Hydroxyphenyl)-arachidonoyl amide
  • HY-122109A
    Levonantradol hydrochloride
    		Agonist
    Levonantradol (l-Nantradol) hydrochloride is an analog of delta (9)-tetrahydrocannabinol. Levonantradol acting as a potent anti-analgesic agent.
    Levonantradol hydrochloride
  • HY-136238
    PM226
    		Agonist
    PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
    PM226
  • HY-103326
    NIDA-41020
    		Antagonist
    NIDA-41020 is a potent and selective cannabinoid receptor 1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET).
    NIDA-41020
  • HY-162298
    γ-Linolenoyl monoethanolamide
    γ-Linolenoyl monoethanolamide, a kind of fatty N-acyl ethanolamine, is an endocannabinoid.
    γ-Linolenoyl monoethanolamide
  • HY-P1397
    RVD-Hpα
    		Agonist
    RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2.
    RVD-Hpα
  • HY-105238
    JHU-75528
    JHU-75528 is a novel ligand of the cannabinoid receptor (CB1). JHU-75528 can be used in the research of imaging CB1 receptor.
    JHU-75528
  • HY-103341
    UCM707
    		Inhibitor
    UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide.
    UCM707
  • HY-131995
    O-Arachidonoyl glycidol
    		Inhibitor
    O-Arachidonoyl glycidol (compound 1) is a 2-arachidonoylglycerol (2-AG) analog. O-Arachidonoyl glycidol inhibits cytosolic 2-oleoylglycerol (2-OG) hydrolysis with an IC50 value of 4.5 µM. O-Arachidonoyl glycidol blocks 2-OG hydrolysis in membrane fractions and anandamide hydrolysis with IC50s of 19, 12 µM, respectively.
    O-Arachidonoyl glycidol
  • HY-151105
    CBR Agonist-1
    		Agonist
    CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases.
    CBR Agonist-1
  • HY-120953
    GAT228
    		Agonist
    GAT228, the enantiomer of GAT211, is an allosteric cannabinoid receptor 1 (CB1) ligand.
    GAT228
  • HY-117403
    AB-FUBICA
    		Agonist
    AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC50 values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms.
    AB-FUBICA
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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