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-B1161A
    S-Methoprene
    		Antagonist 98.58%
    S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [3H]CP-55940 to the CB1 receptor (IC50: 19.31 μM).
    S-Methoprene
  • HY-113204
    N-Oleoyl glycine
    		Activator ≥99.0%
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
    N-Oleoyl glycine
  • HY-110036
    GW-405833
    		Agonist 99.12%
    GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain.
    GW-405833
  • 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-B1739
    Pregnenolone monosulfate
    		Inhibitor 99.22%
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate 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 can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
    Pregnenolone monosulfate
  • HY-16642A
    LY2828360
    		Agonist 99.50%
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
    LY2828360
  • HY-111110
    Olorinab
    		Agonist 99.29%
    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
    Olorinab
  • HY-13505
    AM281
    		Antagonist ≥99.0%
    AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.
    AM281
  • HY-156831
    Lixosicone
    		Inhibitor 99.39%
    Lixosicone is a signaling-specific inhibitor of the cannabinoid receptor 1 (CB1-SSi). Lixosicone plays an important role in Cannabis use disorder (CUD).
    Lixosicone
  • HY-110028
    Leelamine hydrochloride
    		Agonist 99.06%
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
    Leelamine hydrochloride
  • HY-103335
    O1918
    		Antagonist
    O1918 is a selective non-CB1 receptor and GPR18 antagonist.
    O1918
  • 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-14791A
    (±)-Ibipinabant
    		Antagonist 99.30%
    (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
    (±)-Ibipinabant
  • HY-128872
    Etrinabdione
    		Agonist 99.16%
    Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity.
    Etrinabdione
  • HY-131004
    CB2R PAM
    		Agonist 98.46%
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.
    CB2R PAM
  • HY-148137
    CB1 agonist 1
    		Agonist 99.84%
    CB1 agonist 1 (compound 22) is an agonist of CB1. CB1 agonist 1 shows affinity to CB1 receptor with an pIC50 value of 5.7. CB1 agonist 1 can be used for the research of brain disorders.
    CB1 agonist 1
  • HY-110036A
    GW405833 hydrochloride
    		Agonist 99.59%
    GW-405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 hydrochloride also behaves as a noncompetitive CB1 antagonist. GW-405833 hydrochloride suppresses inflammatory and neuropathic pain.
    GW405833 hydrochloride
  • HY-B0151S2
    Pregnenolone-d4-1
    		Inhibitor 99%
    Pregnenolone-d4-1 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>-1
  • HY-116418
    Virodhamine
    		Modulator ≥98.0%
    Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases.
    Virodhamine
  • HY-112340
    CB1 antagonist 4
    		Antagonist 99.00%
    CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects.
    CB1 antagonist 4
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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