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. 2022 Oct 1;14(10):2102. doi: 10.3390/pharmaceutics14102102

Figure 2.

Figure 2

Effect of Rp-8-Br-PET-cGMPS and related cGMP analogues on retinal CNG channels. (A,B) Efficacy of 8-Br-cGMP, PET-cGMP, 8-Br-PET-cGMP and Rp-8-Br-PET-cGMPS when activating rod and cone CNG channels. The currents measured at +100 mV, in the presence of either 1 mM 8-Br-cGMP or 3 mM of the other cGMP analogues, were related to the maximal current induced by saturating cGMP (3 mM for rod and 1 mM for cone CNG channels; n = 4–11). The gray symbols represent individual measurements. (C,D) Concentration–activation relationships for rod and cone CNG channels in the presence of cGMP (black), 8-Br-cGMP (gray), cGMP + 8-Br-PET-cGMP (50 µM, blue) and cGMP + Rp-8-Br-PET-cGMPS (50 µM, orange). The data points representing means of several experiments were fitted with Equation (1). (E,F) Rp-8-Br-PET-cGMPS-inhibitory effect on CNG channels in the presence of 100 µM and 20 µM cGMP for rod and cone CNG channels, respectively. The experimental data points representing means of several measurements were fitted with Equation (2) (n = 8–16 for rod; n = 5–12 for cone; for EC50, H, and n, see Table S1).