TRPV1 - "Heat activation of TRPV1 on Nanion's Patchliner"
Patchliner application note: (0.5 MB)
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1), is a ligand-gated, non-selective cation channel widely expressed in the peripheral and central nervous system. The TRPV1 channel can be activated by a number of physical and chemical stimuli, including capsaicin (the active ingredient in chili peppers), noxious heat (typically >42˚C) and low pH. The TRPV1 channel is putatively involved in the perception and transmission of painful stimuli. Importantly, this channel is proposed to underlie many chronic pain states including inflammation, neuropathic pain and cancer pain, amongst others. These types of pain states are currently poorly managed by the pain medications available and this has led the pharmaceutical industry to seek novel targets for pain management, such as TRPV1. However, TRPV1 antagonists have so far failed in clinical trials due to an undesirable increase in core body temperature resulting in hyperthermia. From these studies, it is proposed that tonically active TRPV1 channels are involved in maintaining normal body temperature and this could have significant influences on drug design. Finding novel compounds with differing effects on capsaicin activation and heat activation may be crucial in the discovery of lead compounds for the treatment of pain and other disease states. Here we present data collected on the 4-channel Patchliner with temperature control showing the potential use of the Patchliner® to record capsaicin and heat activation of TRPV1 channels and subsequent block by ruthenium red (RR).