CB1/2 agonist 2

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

hCB2-R:1.2 nM (Ki)

hCB1-R:3.5 nM (Ki)

CB1/2 agonist 2 (compound 23) (1 µM, 24-72 h) exhibits a very low cytotoxic potential in Hep-G2 cells[1]. CB1/2 agonist 2 (0-10 µM) shows a slight but significant inhibition of [35S]GTPγS binding to hCB2-CHO cell membranes, with a mean EC50 of 397.90 nM and a mean Emax value of -17.81%[1]. Cell Cytotoxicity Assay[1] Cell Line: Human hepatoblastoma (Hep-G2) cells Concentration: 1 µM Incubation Time: 24, 48 or 72 h Result: Exhibited a very low cytotoxic potential, as Hep-G2 cell viability was comparable to controls after 24-72 h of treatment.

CB1/2 agonist 2 (compound 23) (0-6 mg/kg, IP, once) significantly reduces the late phase of formalin-induced nocifensive behaviour at 6 mg/kg[1]. Animal Model: Male CD-1 outbred mice (40-45 g)[1] Dosage: 0, 1, 3, and 6 mg/kg Administration: IP, once, 10 min before the formalin or saline injection Result: Significantly reduced the late phase of formalin-induced nocifensive behaviour at the highest dose (6 mg/kg, i.p.), whereas no effect was produced by doses of 1 and 3 mg/kg.

[1]. Brizzi A, et al. Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. Bioorg Med Chem. 2020 Jun 1;28(11):115513.