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. Author manuscript; available in PMC: 2018 Jun 8.
Published in final edited form as: J Med Chem. 2017 Apr 28;60(11):4680–4692. doi: 10.1021/acs.jmedchem.7b00304

Figure 3.

Figure 3

Compounds 4m–4p activated TRPC6 expressed in HEK293 cells. (A–E) Compounds 4m–4p were synthesized as described in the text and tested in the Ca2+ assay using Fluo8-loaded TRPC6 cells. (A–D) Representative traces of [Ca2+]i rise, as indicated by the Fluo8 fluorescence increase, evoked by varying concentrations of 4m (A), 4n (B), 4o (C), or 4p (D). (E) Summary data for (A–D) and the fits by the Hill equation. (F–J) Compounds 4m–4p were tested on TRPC6 cells in whole-cell recordings. The bath contained 0.1 mM Ca2+, and the pipet solution had 400 nM free Ca2+ buffered by BAPTA. (F–I) Representative current traces at +100 mV (red traces) and –100 mV (blue traces) in response to consecutive applications of increasing concentrations of 4m (F), 4n (G), 4o (H), or 4p (I) (upper panels) and I–V curves for selected compound concentrations (lower panels). (J) Summary data for (F–I) and the fits by the Hill equation.