CB1/2 agonist 1

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.

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 K_is 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.