Fig. 3. DiC8-PIP2 is a partial potentiator of TRPV1 activity.
a,b, VBP with diC8-PIP2 bound in the closed conformation (a) and the dilated conformation (b). c, Top-down view of the TRPV1 pore in the closed conformation (transparent green) and the dilated conformation (dark green). M644 (blue) of the selectivity filter is highlighted. d, Left: pore profile of TRPV1 in the dilated conformation. Right: pore radii of closed (black) and dilated (green) states. e, Schematic of the pore movements demonstrating the dilation of the upper portion of the pore and constriction of the lower portion. f, Top-down view of TRPV1 showing the binding of DOPC (blue) and cholesterol (yellow). g, Top: schematic showing excised inside-out patch clamp recording configuration. Bottom: sample TRPV1 currents evoked by application of control (bathing) solution, 100 µM DiC8-PIP2, or 100 µM DiC8-PIP2 plus 10 µM antagonist AMG-9810. h, Summary of current–voltage relationships showing that DiC8-PIP2 reliably activates TRPV1. Data are graphed as mean ± s.e.m., patch clamp recordings n = 10.