Acid-sensing ion channels (ASICs) are members of the amiloride-sensitive epithelial Na⁺-channel/degenerin superfamily (ENaC/DEG). These ligand-gated ion channels are activated by protons, which are released during tissue acidosis (increase in extracellular acidity). Tissue acidosis, which is evidenced by a drop in extracellular pH, occurs in many acute and chronic pain conditions including inflammation, angina, stroke, ischemic heart disease, arthritis, cancer and traumatic injuries. Protons have been shown to induce pain in humans and it is believed this signal may be mediated by ASICs.

Fig. 1 Pharmacology of acid-sensing ion channels (ASICs) in human cortical neurons

This family of channels consists of six isoforms:

• ASIC1a

• ASIC1b

• ASIC2a

• ASIC2b

• ASIC3

• ASIC4

Of the six ASIC subunits, ASIC1 (1a/1b) and ASIC3 are attractive targets for the treatment of pain since primary sensory neurons are highly enriched with these channels. These primary afferent fibers are nociceptors that detect and signal painful sensations from the periphery to the brain. ASIC1a and ASIC3 are activated by an acidity range (pH 7.0-6.0) observed in several acute and chronic pain conditions. Moreover, ASIC3 is particularly sensitive to lactic acidosis and thus is considered to be an important component of acid-induced pain response during cardiac and muscle ischemia.

Here in Creative Bioarray, we provide target screening on a series of ASICs related to multiple diseases.

Reference

1. Li M, et al. Acid-sensing ion channels in acidosis-induced injury of human brain neurons. J Cereb Blood Flow Metab. 2010; 30: 1247–1260.

Related Section

• Sodium Channels
• Calcium Channels
• Potassium Channels
• Chloride Channels
• TRP Channels
• ATP gated P2X Channels
• Nicotinic Acetylcholine Receptors
• Ionotropic Glutamate-gated Receptors
• GABAa Receptors
• Glycine Receptors
• 5-HT Receptors3
• Cystic Fibrosis Transmembrane Conductance Regulators (CFTR)
• Other Ion Channels