Yc. Lo et al., EFFECT OF CAPSAICIN ON MEMBRANE CURRENTS IN CULTURED VASCULAR SMOOTH-MUSCLE CELLS OF RAT AORTA, European journal of pharmacology. Environmental toxicology and pharmacology section, 292(3-4), 1995, pp. 321-328
The application of capsaicin (1 mu M) produced a minor relaxant effect
in endothelium-denuded rat aortae. However, capsaicin caused a greate
r relaxation of blood vessels precontracted with high K+ or phenylephr
ine. The effects of capsaicin on the ionic currents were also examined
in A7r5 vascular smooth muscle cells. The tight-seal whole-cell volta
ge clamp technique was used. Capsaicin inhibited the Ba2+ inward curre
nt (I-Ba) through the voltage-dependent L-type Ca2+ channel in a conce
ntration-dependent fashion, whereas calcitonin gene-related peptide an
d phenylephrine produced a minor increase in I-Ba. Capsaicin did not a
lter the overall shape of current-voltage relationship of I-Ba. Howeve
r, capsaicin (3 mu M) Shifted the quasi-steady-state inactivation curv
e of I-Ba to more negative membrane potential by about 5 mV. These eff
ects of capsaicin on I-Ba were reversible. In addition, capsaicin had
inhibitory effects on voltage dependent K+ currents. These results sug
gest that inhibition of the voltage-dependent L-type Ca2+ channel is i
nvolved in the capsaicin-induced relaxation of the vascular smooth mus
cle, whereas capsaicin-induced inhibition of voltage-dependent K+ chan
nels might produce an increase in cell excitability.