Add time:08/27/2019         Source:sciencedirect.com

The effects of ARVANIL (cas 128007-31-8) (N-arachidonoyl-vanillyl-amine), a structural hybrid between capsaicin and anandamide, on ion currents in a mouse neuroblastoma and rat glioma hybrid cell line, NG108-15, were examined with the aid of the whole-cell voltage-clamp technique. Arvanil (0.2–50 μM) caused an inhibition of voltage-dependent L-type Ca2+ current (ICa,L) in a concentration-dependent manner. Arvanil produced no change in the overall shape of the current–voltage relationship of ICa,L. The ic50 value of arvanil-induced inhibition of ICa,L was 2 μM. Arvanil (5 μM) could shift the steady-state inactivation curve of ICa,L to a more negative potential by approximately −15 mV. No effect of arvanil (20 μM) on delayed rectifier K+ current (IK(DR)) was observed; however, capsaicin (20 μM), glyceryl nonivamide (20 μM) and capsinolol (20 μM) suppressed it significantly. Arvanil (20 μM) caused a slight reduction in the amplitude of erg (ether-à-go-go-related)-mediated K+ current (IK(erg)) without modifying the activation curve of this current, while capsaicin and glyceryl nonivamide were more effective in suppressing IK(erg). Under current-clamp configuration, arvanil decreased the firing frequency of action potentials. Arvanil-mediated inhibition of ICa,L appeared to be independent of its binding to either vanilloid or cannabinoid receptors. The channel-blocking properties of arvanil may, at least in part, contribute to the underlying mechanisms by which it affects neuronal or neuroendocrine function.

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