Overview
- Shintaku, K. et al. (2011) Br. J. Pharmacol. 165, 1476.
Alomone Labs Capsiate activates TRPA1 channels expressed in HEK-293 cells.Dose-response curve for the activation of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Calcium signal was apparent with 50 and 100 µM Capsiate (#C-255).
Transient receptor potential vanilloid channels (TRPV) are members of the TRP channel superfamily. They are involved in many sensory processes such as pain, temperature and hearing1. Transient receptor potential ankyrin 1 (TRPA1) is a non-selective ion channel, which is expressed in nociceptor sensory neurons and transduces chemical, inflammatory, and neuropathic pain signals. Numerous non-reactive compounds and electrophilic compounds, such as endogenous inflammatory mediators and exogenous pungent chemicals, can activate TRPA12.
Capsiate is a natural agonist of TRPA1 and TRPV1 channels with an effective concentration of 1-100 μM and an EC50 of 3 μM when binding to TRPA1. Capsiate is produced by a non-pungent cultivar of red pepper called Capsicum annuum L and is hypothesized to enhance energy metabolism by activating the sympathetic system and suppressing inflammation3.
Capsiate has also been found to suppress body fat accumulation in mice through the upregulation of uncoupling proteins. Uncoupling proteins play an important role in body weight maintenance, thermoregulation and energy expenditure4. The magnitude of the long-term weight loss effectiveness of capsaicin in humans has not been clearly demonstrated and further research is required in its relation to combating obesity5.
