Capsazepine

138977-28-3

C19H21ClN2O2S

DMSO : >= 50 mg/mL (132.66 mM)

Membrane Transporter/Ion Channel; Neuronal Signaling

Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with IC₅₀ of 562 nM. IC50 & Target: TRPV1 receptor^[1] In Vitro: Capsazepine (50 uM) optimally enhances the upregulation of (death receptors) DRs without affecting cell viability HCT116 cells. Capsazepine (30-50 uM) induces ROS generation and ROS mediate Capsazepine-induced DR5 upregulation in HCT116 cells^[1]. Capsazepine (1-100 uM, 45 min preincubation) inhibits the evoked CGRP-LI release. Capsazepine (3-100 uM) prevents low pH- and capsaicin-induced CGRP-LI release from rat soleus muscle at concentrations which do not affect the release evoked by KCl. Capsazepine (3-100 uM, without 10 uM) produces a nonspecific inhibitory effect on CGRP-LI release from peripheral endings of the capsaicin-sensitive primary afferent neurone^[2]. In Vivo: Capsazepine (15 mg/kg, s.c.) prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine attenuates lung injury evidenced by reduction on collapsed area of the lung parenchyma induced by LPS^[3].