The TRPV1 channel functions as a pain and temperature sensor in mammalians.

Capsazepine blocks the activation of TRPV1 channels by other chemicals, but not by other painful stimuli such as heat.

Depending on the pharmacological assay, the IC50 is in the nanomolar to low micromolar range.

[6] Capsazepine was discovered by a research group working for Novartis.

[7] By incorporation of an azobenzene unit, a photoswitchable version of capsazepine (AC4) was developed in 2013 that allows for optical control of TRPV1 channels with light.