CB1/2 agonist 1 |
| カタログ番号GC71002 |
CB1/2 agonist 1 は強力であり、cb1rとcb2rでそれぞれ56.15,11.63 nmのec50を有する血液脳関門cb 1/2アゴニストである。
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Cas No.: 2986688-90-6
Sample solution is provided at 25 µL, 10mM.
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CB1/2 agonist 1 (compound B2) (10 µM) inhibits AEA hydrolysis with an IC50 of 5.9 µM for FAAH[1].
CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively[1].
CB1/2 agonist 1 (10 µM) shows anti-inflammatory effect and significantly decreases the secretion of IL-1β and IL-6, increases the release of anti-inflammatory IL-10 to 483.7% in LPS-activated BV-2 cells[1].
CB1/2 agonist 1 (1, 10 µM) inhibits 4-AP-evoked glutamate release[1].
CB1/2 agonist 1 (5-50 mg/kg) dose-dependently relieves neuropathic pain in a mouse model of oxaliplatin-induced neuropathic pain[1].
References:
[1]. Arena C, et al. The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. Eur J Med Chem. 2020 Dec 15;208:112858.
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