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].
References:
- [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 Related Products (108)
Related Products (108)
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Bay 59-3074
0 ImagesBay 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.
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Noladin ether
0 ImagesCat. No.: HY-110014CAS No.: 222723-55-9Noladin 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.
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CB2R/FAAH modulator-3
0 ImagesCB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
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Docosatetraenylethanolamide
0 ImagesSynonyms: DEADocosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system.
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MJ15
0 ImagesCat. No.: HY-103327CAS No.: 944154-76-1MJ15 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.
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AM9405
0 ImagesCat. No.: HY-112707CAS No.: 3032946-55-4AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC50s of 45.71 and 0.076 nM, respectively.
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Isopropyl dodec-11-enylfluorophosphonate
0 ImagesCat. No.: HY-148909CAS No.: 623114-64-7Synonyms: IDEFPIsopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM).
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(R)-SLV 319
0 ImagesCat. No.: HY-121616CAS No.: 656827-86-0(R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319
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RTICBM-189
0 ImagesRTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats.
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(±)5(6)-EET Ethanolamide
0 ImagesCat. No.: HY-172568(±)5(6)-EET Ethanolamide is a metabolite of Anandamide (HY-10863) generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.
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LY320135
0 ImagesCat. No.: HY-W011040CAS No.: 176977-56-3LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
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PROTAC CB1R Degrader-1
0 ImagesCat. No.: HY-178176PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research.
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O-2050
0 ImagesCat. No.: HY-133533CAS No.: 1883545-42-3O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice.
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CB1R agonist 1
0 ImagesCat. No.: HY-168997CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating Gi/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain.
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CB1 antagonist 6
0 ImagesCat. No.: HY-178857CB1 antagonist 6 (Compound 11jE2) is an orally active CB1R antagonist, with an IC50 value of 23 nM. CB1 antagonist 6 significantly reduces food intake and body weight, improves glucose tolerance and insulin resistance, and decreases serum ALT and AST levels in diet-induced obese (DIO) mice, demonstrating hepatoprotective effects. CB1 antagonist 6 can be used for the study of metabolic syndrome (obesity, diabetes).
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CB1R Allosteric modulator 4
0 ImagesCat. No.: HY-150057CAS No.: 2633686-53-8CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.
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BAY 38-7271
0 ImagesCat. No.: HY-119744CAS No.: 212188-60-8BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
