Skip to main content
Figure 2 | Molecular Pain

Figure 2

From: Analgesic effect of a mixed T-type channel inhibitor/CB2 receptor agonist

Figure 2

Pharmacological and biophysical properties of NMP-181 block of T-type calcium channels. (A) concentration dependence of NMP-181 inhibition of the CaV3.2 peak current amplitude. The data were fitted with a Hill equation. The half-maximal inhibitory concentration (IC50) from the fit was 4.6 μM and the Hill coefficient was 2.1. Numbers in parentheses reflect numbers of experiments for each concentration point. (B) representative time course of the development of and recovery from NMP-181 (30 μM) inhibition. (C), NMP-181 (10 μM) did not show selectivity on CaV3 channels, as illustrated in the histogram and (D) representative traces from NMP-181 inhibition on CaV3.1, 3.2 and 3.3 currents. Statistical significance was determined by one-way ANOVA followed by a Dunnett’s test, when the data were compared to those from CaV3.2 group. (E) normalized current–voltage relations of CaV3.2 current before and after application of 10 μM NMP-181. The half-activation potentials were -32.7 ± 2.0 mV and -38.4 ± 2.8 mV before and after application of NMP-181, respectively (inset, P < 0.05, paired t test). (F) steady-state inactivation curve obtained from CaV3.2 channels before and after application of 10 μM NMP-181. The half-inactivation potentials were -56.0 ± 2.8 mV and -64.1 ± 4.0 mV before and after the treatment with NMP-181, respectively (inset, P < 0.01, paired t test).

Back to article page