CB1
Cannabinoid receptor CB1 (CB1R) is a G protein-coupled receptor expressed mainly by neurons in the brain, spinal cord, peripheral nervous system, and enteric nervous system[1]. Mechanistically, CB1R stimulates Gi/o-dependent signaling and regulates cAMP output, while CB1R-mediated ERK activation in neuronal cells involves receptor tyrosine kinase transactivation, PI3K, Src, PKA, and PP1/PP2A signaling modules[2][3]. In disease models, CB1R antagonists attenuated doxorubicin-induced oxidative/nitrosative stress, MAPK activation, and cardiomyocyte death, and CB1R antagonism reduced alcohol-induced hippocampal pyroptosis signaling[4][5]. Compared with CB2, which appears mainly in immune cells, CB1R shows stronger neuronal and enteric distribution and mediates gut motility, intestinal secretion, and cholinergic neurotransmission through peripheral CB1 receptors[1]. For experimental applications, selective CB1 antagonists or inverse agonists such as SR141716A, AM251, AM281, and rimonabant help test CB1R-dependent signaling, whereas CB1-selective or cannabinoid agonists such as ACEA, HU210, anandamide, and hemopressin support pathway analysis in vascular, cardiac, neuronal, and feeding models[4][5][6][7].
Références:
- [1]. Vigna SR. Cannabinoids and the gut. Gastroenterology. 2003 Sep;125(3):973-5. doi: 10.1016/s0016-5085(03)01134-x. PMID: 12949741. et al. Cannabinoids and the gut. Gastroenterology. 2003 Sep;125(3):973-5. [Content Brief]
- [2]. Eldeeb K, et al. CB1 cannabinoid receptor-mediated increases in cyclic AMP accumulation are correlated with reduced Gi/o function. J Basic Clin Physiol Pharmacol. 2016 May 1;27(3):311-22. [Content Brief]
- [3]. Dalton GD, et al. Cannabinoid CB1 receptors transactivate multiple receptor tyrosine kinases and regulate serine/threonine kinases to activate ERK in neuronal cells. Br J Pharmacol. 2012 Apr;165(8):2497-511. [Content Brief]
- [4]. Mukhopadhyay P, et al. CB1 cannabinoid receptors promote oxidative stress and cell death in murine models of doxorubicin-induced cardiomyopathy and in human cardiomyocytes. Cardiovasc Res. 2010 Mar 1;85(4):773-84. [Content Brief]
- [5]. Zhang D, et al. Cannabinoid 1 Receptor Antagonists Play a Neuroprotective Role in Chronic Alcoholic Hippocampal Injury Related to Pyroptosis Pathway. Alcohol Clin Exp Res. 2020 Aug;44(8):1585-1597. [Content Brief]
- [6]. Hermans A, et al. A 3D-Printed and Freely Available Device to Measure the Zebrafish Optokinetic Response Before and After Injury. Zebrafish. 2024 Apr;21(2):144-148. [Content Brief]
- [7]. Dodd GT, et al. The peptide hemopressin acts through CB1 cannabinoid receptors to reduce food intake in rats and mice. J Neurosci. 2010 May 26;30(21):7369-76. [Content Brief]
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CB1 Produits associés (108)
Produits associés (108)
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GW405833 hydrochloride
0 ImagesSynonyms: L768242 hydrochlorideGW405833 (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).
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(R)-Methanandamide
0 ImagesCat. No.: HY-101389CAS No.: 157182-49-5Synonyms: AM-356
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Ibipinabant
0 ImagesSynonyms: SLV319; BMS-646256
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Eicosapentaenoyl ethanolamide
0 ImagesEicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant.
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CB1/2 agonist 1
0 ImagesCB1/2 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.
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Dihomo-γ-Linolenoyl Ethanolamide
0 ImagesDihomo-γ-Linolenoyl Ethanolamide, an endocannabinoid, is a cannabinoid (CB) receptor agonist with Kis of 857 nM and 598 nM for human recombinant CB1 and CB2 receptors, respectively.
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CB1 antagonist 4
0 ImagesCB1 antagonist 4 (compound 8) is a selective cannabinoid receptor 1 (CB1) inverse agonist with an IC50 of 8.5 nM for human CB1. CB1 antagonist 4 shows selective for CB1 over CB2 receptors (IC50 of 604.9 nM). CB1 antagonist 4 inhibits GTP binding to CB1-overexpressing cell membranes with an EC50 of 18.5 nM.
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CB1 inverse agonist 2
0 ImagesCB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model.
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AZD1940
0 ImagesAZD1940 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.
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Zevaquenabant
0 ImagesSynonyms: (S)-MRI-1867Zevaquenabant ((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).
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Auriculasin
0 ImagesAuriculasin is an anticancer agent that inhibits VEGFR2, PI3K/AKT/mTOR, MAPK. Auriculasin can inhibit cell proliferation, induce cell apoptosis, and inhibit angiogenesis, and promotes mitochondrial oxidative stress and ferroptosis. Auriculasin is also active at the cannabinoid receptor CB1 with an IC50 of 8.92 μM. Auriculasin can be used in cancer research, especially related diseases such as prostate cancer and non-small cell lung cancer, as well as research on the development of anti-angiogenic drugs.
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JTE-907
0 ImagesJTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.
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URB447
0 ImagesURB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity.
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2-Palmitoylglycerol
0 ImagesSynonyms: 2-Palm-Gl2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.
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ANEB-001
0 ImagesCat. No.: HY-148176CAS No.: 791848-71-0ANEB-001 is an orally active CB1 inhibitor, can be used to research acute cannabinoid intoxication.
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BPRCB1184
0 ImagesSynonyms: CB1-IN-1BPRCB1184 is a peripherally restricted 1-type cannabinoid receptor (CB1) antagonist, whose activity is associated with the regulation of obesity-related endocannabinoid system. BPRCB1184 regulates the activity of the endocannabinoid system, promotes lipid mobilization, reduces triglyceride storage, improves glucose metabolism, decreases food intake and body weight, while enhances insulin resistance and improves blood lipid levels. BPRCB1184 can be used in obesity-related research.
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L759633
0 ImagesL759633 is a potent and selective agonist of cannabinoid receptor (CB2) receptor, with Kis of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production.
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N-Arachidonoylserotonin
0 ImagesSynonyms: Arachidonyl serotonin; AA-5-HTN-Arachidonoylserotonin (Arachidonyl serotonin) is a dual FAAH inhibitor and TRPV1 antagonist. N-Arachidonoylserotonin blocks Anandamide (HY-10863) hydrolysis, increases brain Anandamide levels, and promotes CB1 receptor signaling in the dorsal hippocampus. N-Arachidonoylserotonin normalizes HPA axis dysregulation, reduces plasma corticosterone levels, and induces anxiolytic-like effects in mice. N-Arachidonoylserotonin reverses behavioral despair, inhibits contextual fear memory retrieval, and produces dose-dependent antinociceptive effects in rodents. N-Arachidonoylserotonin inhibits intestinal motility. N-Arachidonoylserotonin can be used to study stress-related disorders, traumatic memory and related psychiatric disorders, pain, and intestinal motility disorders.
