How do I activate TRPV1 naturally?

TRPV1 is activated by a wide variety of different stimuli including heat, protons (pH < 5.9) (8, 19), capsaicin the irritant compound in hot chilies (10), allicin and diallyl sulfides from garlic (20, 21), peperine from black pepper (22), and gingerol from ginger (23).

What does capsaicin do to TRPV1?

TRPV1 is a non-selective cation channel; when it is activated by capsaicin, sodium and calcium ions flowing through TRPV1 into the cell to depolarize nociceptive neurons, leading to action potential firing and finally the sensation of spiciness (Caterina et al., 1997).

What triggers TRPV1?

TRPV1 is best known for its function in nociceptive neurons, detecting noxious heat and pain. It is activated by heat and capsaicin, the pungent compound in chili peppers [76]. There is functional expression of TRPV1 in the brain and sensory neurons [77].

Are there any antagonists to the drug TRPV1?

Identified antagonists include the competitive antagonist capsazepine and the non-competitive antagonist ruthenium red. These agents could be useful when applied systemically. Numerous TRPV1 antagonists have been developed by pharmaceutical companies.

What are some substances that sensitize the TRPV1 receptor?

Some substances such as bradykinin, nerve growth factor and protons have been reported to sensitize the TRPV1 receptor. Activation of TRPV1 results in the release of pro-nociceptive peptides, which decreases when treated with TRPV1 antagonists.

Which is the most selective TRPC4 channel inhibitor?

ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels.

How is the activity of TRPV1 regulated in the body?

Importantly, TRPV1 activity is also subject to regulation by a host of intracellular signaling cascades such as G-protein coupled receptor signaling, that are implicated in the responses to algogenic agents, inflammatory mediators and injury.