Fig. 1.
Chemical structure of compound JWX-A0108 and its allosteric and dose-dependent activation of human α7 nAChR channels expressed in Xenopus oocytes. a Chemical structure of compound 6-(2-chloro-6-methylphenyl)-2-((3-fluoro-4-methylphenyl)amino)thiazolo[4,5-d]pyrimidin-7(6H)-one (JWX-A0108, molecular weight of 400.06). b Representative α7 currents recorded from an oocyte expressing human α7 nAChR in response to 100 µM ACh in the absence or presence of different concentrations of JWX-A0108 (0.1–30 µM). c Concentration–response relationship for JWX-A0108. Peak current amplitudes were normalized to the amplitude of current elicited by 100 µM ACh alone, and EC50 = 4.35 ± 0.12 µM, fold increase: 23.7 ± 2.36, and nHill = 2.08 ± 0.03, n = 5 for all data. d Fold-increase in α7 nAChR current, α3β4 nAChR current, and α4β2 nAChR current in the presence of 100 μM or 5-HT3A receptor current evoked by 10 μM 5-HT after incubation with 10 μM JWX-A0108, n = 5 for all experiments. Data are expressed as the means ± SEM