1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110206
    AM6545
    Antagonist 98.74%
    AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications.
    AM6545
  • HY-10871
    Otenabant
    Antagonist 99.23%
    Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
    Otenabant
  • HY-101388
    AM404
    Inhibitor ≥99.0%
    AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Neuroprotective Effect.
    AM404
  • HY-N6932
    Voacamine
    Antagonist 99.64%
    Voacamine, an indole alkaloid, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
    Voacamine
  • 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-121852
    SCH 336
    Agonist 98.85%
    SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice.
    SCH 336
  • HY-116637
    Tetrahydromagnolol
    Agonist 99.79%
    Tetrahydromagnolol (Magnolignan), the main metabolite of Magnolol, is a potent and selective cannabinoidCB2 receptor agonist (EC50 =170 nM) and GPR55 antagonist. The Ki of Tetrahydromagnolol for CB2 is 416 nM, 20-fold higher than for the CB1 receptor. Magnolol shows antifungal, anti-inflammatory and analgesic effects.
    Tetrahydromagnolol
  • HY-14167
    GW842166X
    Agonist 99.97%
    GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.
    GW842166X
  • 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 99.75%
    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-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-147512
    CB1/2 agonist 1
    Agonist 99.20%
    CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.
    CB1/2 agonist 1
  • HY-117139
    NESS 0327
    Antagonist 99.22%
    NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.
    NESS 0327
  • 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-145604
    Vicasinabin
    Agonist 98.37%
    Vicasinabin (RG7774) is the potent agonist of cannabinoid receptor 2 (CB2). Vicasinabin has the potential for the research of human diseases including chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and other related diseases (extracted from patent US20130116236A1).
    Vicasinabin
  • HY-162617
    PSB-KK1415
    Agonist 99.92%
    PSB-KK1415 is a selective agonist for human orphan G protein-coupled receptor GPR18, with EC50 of 19.1 nM.
    PSB-KK1415
  • 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-113421
    Linoleoyl ethanolamide
    ≥98.0%
    Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1(CB1)and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time.
    Linoleoyl ethanolamide
Cat. No. Product Name / Synonyms Application Reactivity

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