体外研究
QX-314 bromide exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels (TRPV1) in vitro .
QX-314 bromide (1–60 mM) directly activates TRPV1 in a concentration-dependent manner.
QX-314 bromide (≥ 30 mM) produces oocyte membrane blackening and cell death .
QX-314 bromide inhibits calcium currents in hippocampal CA1 pyramidal neurons intracellular, and the low-threshold (T-type) Ca
2+
currents are on average < 10% of control amplitude .
QX-314 bromide shifts the current-voltage relationships (I-Vs) in the positive voltage direction due to the presence of intracellular Br- .
体内研究
QX-314 bromide (1.6 mg/kg; i.c.) abolishes responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin.
Animal Model:
Male Sprague-Dawley rats (250-290 g)
Dosage:
1.6 mg/kg
Administration:
Intracutaneous injection
Result:
Abolished responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin.
