Abstract
UCL-2077 (triphenylmethylaminomethyl)pyridine) was previously reported to suppress slow afterhyperpolarization in neurons. However, the information with respect to the effects of UCL-2077 on ionic currents is quite scarce. The addition of UCL-2077 decreased the amplitude of erg-mediated K(+) current (I(K()(erg))) together with an increased deactivation rate of the current in pituitary GH(3) cells. The IC(50) and K(D) values of UCL-2077-induced inhibition of I(K()(erg)) were 4.7 and 5.1 μM, respectively. UCL-2077 (10 μM) distinctly shifted the midpoint in the activation curve of I(K()(erg)) to less hyperpolarizing potentials by 17 mV. Its presence decreased the degree of voltage hysteresis for I(K()(erg)) elicitation by long-lasting triangular ramp pulse. It also diminished the probability of the opening of intermediate-conductance Ca(2+)-activated K(+) channels. In cell-attached current recordings, UCL-2077 raised the frequency of action currents. When KCNH2 mRNA was knocked down, a UCL-2077-mediated increase in AC firing was attenuated. Collectively, the actions elaborated herein conceivably contribute to the perturbating effects of this compound on electrical behaviors of excitable cells.