Transient receptor potential ankyrin 1 and transient receptor potential vanilloid 1 (TRPA1/TRPV1)

Transient receptor potential ankyrin 1 (TRPA1) and transient receptor potential vanilloid 1 (TRPV1) are non-selective cation channels primarily expressed in nociceptive sensory neurons (Julius, 2013). They serve as polymodal sensors for noxious heat (TRPV1), cold (TRPA1), and various chemical irritants, and are known to be co-expressed and form functional heteromeric complexes (Starowicz et al., 2008; Akopian, 2011). These channels play a significant role in chronic pain, neurogenic inflammation, and respiratory conditions like asthma and chronic cough (Nilius & Szallasi, 2014). Therapeutic targeting of these channels, particularly through antagonism, aims to alleviate pain and inflammation, though clinical progress for TRPV1 antagonists has been hindered by side effects such as hyperthermia (Gavva et al., 2008). The interaction between TRPA1 and TRPV1 suggests that dual antagonism or targeting the heteromeric complex may offer enhanced therapeutic efficacy in certain disease states.

Other names

TRPA1-TRPV1 complexTRPA1/V1ANKTM1/VR1Transient receptor potential cation channel subfamily A member 1 and transient receptor potential cation channel subfamily V member 1

Antagonism of TRPA1 and TRPV1 ion channels to inhibit the influx of cations (Ca2+, Na+), thereby reducing neuronal excitability and pain signaling (Julius, 2013; Nilius & Szallasi, 2014).