产品
编 号:F762719
分子式:C21H24BrFN2O2
分子量:435.33
产品类型
结构图
CAS No: 2986688-90-6
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产品详情
生物活性:
CB1/2 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.
体内研究:
CB1/2 agonist 1 (5-50 mg/kg) dose-dependently relieves neuropathic pain in a mouse model of oxaliplatin-induced neuropathic pain.
体外研究:
CB1/2 agonist 1 (compound B2) (10 μM) inhibits AEA hydrolysis with an IC50 of 5.9 μM for FAAH.CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively.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.CB1/2 agonist 1 (1, 10 μM) inhibits 4-AP-evoked glutamate release.