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Results for "

CB1+receptor

" in MedChemExpress (MCE) Product Catalog:

93

Inhibitors & Agonists

2

Peptides

12

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15443
    AM251
    Maximum Cited Publications
    23 Publications Verification

    Cannabinoid Receptor Neurological Disease
    AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC50 of 39 nM [1] .
    AM251
  • HY-B0151
    Pregnenolone
    Maximum Cited Publications
    6 Publications Verification

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    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] . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone
  • HY-B1739
    Pregnenolone monosulfate
    Maximum Cited Publications
    6 Publications Verification

    3β-Hydroxy-5-pregnen-20-one monosulfate

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    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 [1] . Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone monosulfate
  • HY-116637

    Magnolignan

    Cannabinoid Receptor GPR55 Drug Metabolite Infection Neurological Disease Inflammation/Immunology
    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 [1] .
    Tetrahydromagnolol
  • HY-B1161A
    S-Methoprene
    2 Publications Verification

    (+)-Methoprene; (7S)-Methoprene

    Environmental Pollutants Cannabinoid Receptor Others
    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) [1] .
    S-Methoprene
  • HY-N0919
    Yangonin
    1 Publications Verification

    Cannabinoid Receptor NF-κB Autophagy Inflammation/Immunology
    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
  • HY-13505
    AM281
    1 Publications Verification

    Cannabinoid Receptor Neurological Disease
    AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM [1].
    AM281
  • HY-110189
    Pregnenolone monosulfate sodium
    Maximum Cited Publications
    6 Publications Verification

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    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] . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone monosulfate sodium
  • HY-117771
    DO34
    5 Publications Verification

    DAGL Neurological Disease Metabolic Disease
    DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 blocks de novo 2-AG synthesis, and suppresses tonic CB1 receptor activation. DO34 blocks depolarization-induced suppression of excitation and inhibition in the cerebellum and hippocampus. DO34 regulates feeding behavior and locomotor activity in mice. DO34 abolishes AM251-mediated enhancement of parallel fiber-evoked excitatory postsynaptic currents in cerebellar slices from MAGL global knockout mice. DO34 can be used for the research of energy balance disorder and neuroinflammation [1] .
    DO34
  • HY-13288

    Cannabinoid Receptor Neurological Disease
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
    Org 27569
  • HY-113204
    N-Oleoyl glycine
    2 Publications Verification

    Endogenous Metabolite Cannabinoid Receptor Akt Metabolic Disease
    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-10013
    Taranabant
    2 Publications Verification

    MK-0364

    Cannabinoid Receptor Metabolic Disease
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
    Taranabant
  • HY-14791A
    (±)-Ibipinabant
    1 Publications Verification

    (±)-SLV319; (±)-BMS-646256

    Cannabinoid Receptor Metabolic Disease
    (±)-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-110206

    Cannabinoid Receptor Metabolic Disease
    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 [1] .
    AM6545
  • HY-B0151R
    Pregnenolone (Standard)
    5 Publications Verification

    3β-Hydroxy-5-pregnen-20-one (Standard)

    Reference Standards Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (Standard) is the analytical standard of Pregnenolone. This product is intended for research and analytical applications. 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] . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone (Standard)
  • HY-14791
    Ibipinabant
    1 Publications Verification

    SLV319; BMS-646256

    Cannabinoid Receptor Metabolic Disease
    Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic [1] .
    Ibipinabant
  • HY-130311

    2-Monolinolein; 2-Monolinoleoylglycerol

    Cannabinoid Receptor Neurological Disease
    2-Linoleoyl glycerol (2-Monolinolein) is a partial CB1 receptor agonist with a pEC50 of 4.781. 2-Linoleoyl glycerol activates the hCB1 receptor. 2-Linoleoyl glycerol does not induce an increase in intracellular free Ca 2+. 2-Linoleoyl glycerol can be used in the research of neurological disorders [1] .
    2-Linoleoyl glycerol
  • HY-110036

    L768242

    Cannabinoid Receptor Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) [1] .
    GW-405833
  • HY-10013A

    MK-0364 racemate

    Cannabinoid Receptor Neurological Disease
    Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1 [1].
    Taranabant racemate
  • HY-110018

    Cannabinoid Receptor TRP Channel Neurological Disease
    N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM [1]. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM .
    N-Arachidonyldopamine
  • HY-148137
    CB1 agonist 1
    1 Publications Verification

    Cannabinoid Receptor Neurological Disease
    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 [1].
    CB1 agonist 1
  • HY-117139
    NESS 0327
    1 Publications Verification

    Cannabinoid Receptor Neurological Disease
    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 [1].
    NESS 0327
  • HY-110003
    Arachidonylcyclopropylamide
    2 Publications Verification

    ACPA

    Cannabinoid Receptor Neurological Disease
    Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) [1].
    Arachidonylcyclopropylamide
  • HY-103335
    O1918
    1 Publications Verification

    Cannabinoid Receptor Cardiovascular Disease
    O1918 is a selective non-CB1 receptor and GPR18 antagonist.
    O1918
  • HY-118140

    Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    ZCZ011 is a potent and brain-penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain [1].
    ZCZ011
  • HY-110047

    Cannabinoid Receptor Inflammation/Immunology
    CB65 is a potent and high affinity CB2 selective agonist with a Ki value of 3.3 nM. CB65 exhibits a Ki of >1000 nM for CB1 receptor [1].
    CB65
  • HY-141411A

    (S)-MRI-1867

    Cannabinoid Receptor NO Synthase Metabolic Disease
    Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD) [1].
    Zevaquenabant
  • HY-177425

    Cannabinoid Receptor Metabolic Disease
    AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 Ki of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity [1].
    AM11542
  • HY-124283A

    Cannabinoid Receptor Neurological Disease
    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 [1] .
    LEI-101
  • HY-B0151S2

    3β-Hydroxy-5-pregnen-20-one-d4-1

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    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] . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone-d4-1
  • HY-125743

    (S)-Methanandamide

    Cannabinoid Receptor Neurological Disease
    S-1 Methanandamide ((S)-Methanandamide), an Anandamide analog, is a CB1 receptor ligand with a Ki of 173 nM. S-1 Methanandamide inhibits electrically-evoked twitch response in mouse vas deferens with an IC50 value of 230 nM [1].
    S-1 Methanandamide
  • HY-14788

    AVE1625

    Cannabinoid Receptor Metabolic Disease
    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 [1].
    Drinabant
  • HY-112828

    DAGL Neurological Disease Metabolic Disease Inflammation/Immunology
    LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation [1].
    LEI105
  • HY-159161

    Orphan GPCR Inflammation/Immunology Cancer
    PSB-CB-27 is a potent and selective GPR18 inhibitor with an IC50 of 0.65 μM. PSB-CB-27 shows selectivity over Human GPR55, Human CB1 receptor, and Human CB2 receptor. PSB-CB-27 leads to a complete blockade of Δ9-Tetrahydrocannabinol (THC)-induced GPR18 activation. PSB-CB-27 can be used for inflammatory diseases and cancer immunotherapy research [1].
    PSB-CB-27
  • HY-103327

    Cannabinoid Receptor Metabolic Disease
    MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice [1].
    MJ15
  • HY-110014

    Cannabinoid Receptor Neurological Disease
    Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception [1].
    Noladin ether
  • HY-14753

    Cannabinoid Receptor Cardiovascular Disease Metabolic Disease
    Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder [1].
    Rosonabant
  • HY-110189S1

    3β-Hydroxy-5-pregnen-20-one monosulfate-d4 sodium

    Isotope-Labeled Compounds Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate-d4 sodium is the deuterium labeled Pregnenolone monosulfate sodium (HY-110189) . 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] . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone monosulfate-d4 sodium
  • HY-110194

    Endogenous Metabolite Cannabinoid Receptor Neurological Disease
    Virodhamine TFA 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 TFA induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine TFA can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases [1] .
    Virodhamine TFA
  • HY-110036A

    L768242 hydrochloride

    Cannabinoid Receptor Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) [1] .
    GW405833 hydrochloride
  • HY-183113

    Cannabinoid Receptor Neurological Disease
    CB1-receptor agonist-1 is the racemic form of compound ‘1350 and is also a cannabinoid-1 receptor (CB1R) agonist [1].
    CB1-receptor agonist-1
  • HY-128040

    Endogenous Metabolite Cannabinoid Receptor Neurological Disease
    Virodhamine (hydrochloride) is a cannabinoid CB1 receptor partial agonist and cannabinoid CB2 receptor full agonist [1].
    Virodhamine hydrochloride
  • HY-N6097

    Cannabinoid Receptor Neurological Disease
    Amauromine is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist with Ki and Kb values of 178 nM and 66.6 nM, respectively [1].
    Amauromine
  • HY-12606

    Cannabinoid Receptor Metabolic Disease
    BMS-812204 is a highly selective CB-1 receptor antagonist. BMS-812204 is promising for research of obesity and metabolic disorders [1].
    BMS-812204
  • HY-105238

    Cannabinoid Receptor Neurological Disease
    JHU-75528 is a novel ligand of the cannabinoid receptor (CB1). JHU-75528 can be used in the research of imaging CB1 receptor [1].
    JHU-75528
  • HY-110179

    Cannabinoid Receptor Metabolic Disease
    PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity [1].
    PSNCBAM-1
  • HY-114880

    Cannabinoid Receptor Neurological Disease
    AB-FUBINACA 3-fluorobenzyl isomer is a synthetic cannabinoid that belongs to the indole derivatives and has a high affinity for the central CB1 receptors (Ki= 0.9 nM), exhibiting anticonvulsant activity [1].
    AB-FUBINACA 3-fluorobenzyl isomer
  • HY-B0151S

    3β-Hydroxy-5-pregnen-20-one-d4

    Isotope-Labeled Compounds Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone-d4 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] . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
    Pregnenolone-d4
  • HY-B0151S1

    3β-Hydroxy-5-pregnen-20-one-13C2,d2

    Isotope-Labeled Compounds Autophagy Cannabinoid Receptor Endogenous Metabolite TRP Channel Neurological Disease
    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] .
    Pregnenolone-13C2,d2
  • HY-121827
    LH21
    1 Publications Verification

    Cannabinoid Receptor Metabolic Disease
    LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats. , and displays efficacy as a feeding inhibitor [1].
    LH21

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