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 (107)
Related Products (107)
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CB1R Allosteric modulator 3
0 ImagesCB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.
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MDA7
0 ImagesCat. No.: HY-173083CAS No.: 1103840-28-3MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.
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MN-25
0 ImagesCat. No.: HY-124954CAS No.: 501926-82-5MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has Ki of 245 nM and 11 nM for CB1 and CB2. MN-25 has CB2 agonist activity and inhibits TNF-R release in human peripheral blood mononuclear cells in vitro with an IC50 of 33 μM. MN-25 shows efficacy in a mouse acute inflammation model at oral doses up to 50 mg/kg>[1].
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L-759656
0 ImagesCat. No.: HY-110041CAS No.: 174627-56-6L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin (HY-15371)-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.
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CB1/2 receptor-1
0 ImagesCat. No.: HY-164817CAS No.: 1260669-31-5CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.
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CBR Agonist-2
0 ImagesCat. No.: HY-151107CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 and a Ki of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.
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RD-pepcan-11
0 ImagesCat. No.: HY-P11831RD-pepcan-11 is a CB1 receptor agonist. RD-pepcan-11 increases the relative phosphorylation level of ERK1/2. RD-pepcan-11 mediates analgesic effects through interaction with CB1 receptors in a carrageenan-induced mouse inflammatory pain model. RD-pepcan-11 can be used in studies related to inflammatory pain.
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(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide
0 ImagesCat. No.: HY-115428CAS No.: 220556-74-1(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM.
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Dodec-2E-ene-8,10-diynoic acid isobutylamide
0 ImagesCat. No.: HY-N19807CAS No.: 120727-29-9Dodec-2E-ene-8,10-diynoic acid isobutylamide is an alkamide found in Echinacea angustifolia that binds to CB1 (rat Ki = 61.1 μM) and CB2 (mouse Ki = 47.2 μM) cannabinoid receptors. Dodec-2E-ene-8,10-diynoic acid isobutylamide can be used in research on inflammatory diseases.
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CB2R/FAAH modulator-2
0 ImagesCat. No.: HY-152253CAS No.: 2876918-68-0CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
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CB1-receptor agonist-1
0 ImagesCat. No.: HY-183113CAS No.: 3069879-24-6CB1-receptor agonist-1 is the racemic form of compound ‘1350 and is also a cannabinoid-1 receptor (CB1R) agonist.
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R-2 Methanandamide
0 ImagesCat. No.: HY-123594CAS No.: 157182-47-3R-2 Methanandamide (Compound 2) is a cannabinoid Anandamide (HY-10863) analog with a Ki of 119 nM for the cannabinoid receptor (Ki is determined using rat brain membranes with PMSF).
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Amauromine
0 ImagesCat. No.: HY-N6097CAS No.: 88360-87-6Amauromine is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist with Ki and Kb values of 178 nM and 66.6 nM, respectively.
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BNS808
0 ImagesBNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.
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MK-5596
0 ImagesCat. No.: HY-10575CAS No.: 1044586-68-6MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.
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AM12814
0 ImagesCat. No.: HY-178203CAS No.: 3054511-18-8AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.
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O-1812
0 ImagesCat. No.: HY-178698CAS No.: 342882-77-3O-1812 is a selective CB1 ligand. O-1812 is also a very weak AMT inhibitor. O-1812 can be used in the research of chronic pain, migraines, and inflammation.
