TY - JOUR
T1 - Effect of arvanil (N-arachidonoyl-vanillyl-amine), a nonpungent anandamide-capsaicin hybrid, on ion currents in NG108-15 neuronal cells
AU - Lo, Yuk Keung
AU - Chiang, Hung Ting
AU - Wu, Sheng Nan
N1 - Funding Information:
The authors gratefully thank Hui-Fang Li and Yen-Hua Hung for their technical assistance. The authors also thank Pei-Hsuan Lin for initial experiments in measurement of Ca 2+ current. This work was supported by grants from the National Science Council (NSC-91-2320-B075B-003), Kaohsiung Veterans General Hospital (VGHKS90-06, and VGHKS90-73), and VTY Joint Research Program, Tsou’s Foundation (VTY-89-P3-23), Taiwan, ROC.
PY - 2003/2/15
Y1 - 2003/2/15
N2 - The effects of arvanil (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 (0.2-50μM) 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 2μM. Arvanil (5μM) could shift the steady-state inactivation curve of ICa,L to a more negative potential by approximately -15mV. No effect of arvanil (20μM) on delayed rectifier K+ current (IK(DR)) was observed; however, capsaicin (20μM), glyceryl nonivamide (20μM) and capsinolol (20μM) suppressed it significantly. Arvanil (20μM) 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.
AB - The effects of arvanil (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 (0.2-50μM) 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 2μM. Arvanil (5μM) could shift the steady-state inactivation curve of ICa,L to a more negative potential by approximately -15mV. No effect of arvanil (20μM) on delayed rectifier K+ current (IK(DR)) was observed; however, capsaicin (20μM), glyceryl nonivamide (20μM) and capsinolol (20μM) suppressed it significantly. Arvanil (20μM) 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.
UR - https://www.scopus.com/pages/publications/0037441422
UR - https://www.scopus.com/pages/publications/0037441422#tab=citedBy
U2 - 10.1016/S0006-2952(02)01569-1
DO - 10.1016/S0006-2952(02)01569-1
M3 - Article
C2 - 12566085
AN - SCOPUS:0037441422
SN - 0006-2952
VL - 65
SP - 581
EP - 591
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 4
ER -