Reactome | ASIC3 channel blockers bind ASIC3 trimer

ASIC3 channel blockers bind ASIC3 trimer

Stable Identifier

R-HSA-9649963

Type

Reaction [binding]

Species

Homo sapiens

Compartment

plasma membrane, extracellular region

ReviewStatus

5/5

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ASIC3 channel blockers bind ASIC3 trimer

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Acid-sensing ion channels 1, 2, 3 and 5 (ASIC1, 2, 3 and 5, aka amiloride-sensitive cation channels) are a subfamily of the ENaC/Deg superfamily of ion channels. ASICs are low pH-activated Na+-permeable ion channels that are widely expressed in the central and peripheral nervous systems. ASICs act as pH sensors, leading to neuronal excitation when the pH drops. ASICs play important roles in mediating pain sensation in conditions such as stroke, inflammation, arthritis, cancer and migraine. They may additionally control the adverse behavioral and emotional symptoms of chronic pain such as anxiety and depression. ASIC3 channels are mainly expressed in the peripheral nervous system and inhibition of activity of these channels by ASIC3 channel blockers could be a promising tool for pain relief.

The diuretic amiloride, a nonspecific blocker of sodium channels, is a well-known drug that possesses a nonspecific inhibitory effect on ASICs (Ugawa et al. 2002).

Literature References

PubMed ID	Title	Journal	Year
12393854	Amiloride-blockable acid-sensing ion channels are leading acid sensors expressed in human nociceptors Ugawa, S, Ueda, T, Ishida, Y, Nishigaki, M, Shibata, Y, Shimada, S	J. Clin. Invest.	2002
11588175	Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors Voilley, N, de Weille, J, Mamet, J, Lazdunski, M	J. Neurosci.	2001