Ralfinamide mesylate (NW-1029) is a Na+ channel blocker that suppresses tetrodotoxin (TTX)-resistant Na+ currents in small to medium size (C-type) dorsal root ganglia (DRG) neurons about twice as selectively as it blocks TTX-sensitive currents in the same neurons; IC50 values for tonic block of half-maximal inactivated tetrodotoxin-resistant and tetrodotoxin-sensitive currents are 10 μM and 22 μM, respectively. The blocking action of ralfinamide shows frequency and voltage dependence. In experimental animal models of inflammatory and neuropathic pain, systemic administration of ralfinamide elicits anti-nociceptive effects.
產品描述
A Use Dependent Blocker of TTX-resistant and TTX-sensitive NaV Channels
產品形式
Voltage-gated Na+ channels (VGSCs) comprise a large multigene family encoding individual subtypes that can be differentiated on the basis of primary structure, biophysical properties and sensitivity to the neurotoxin tetrodotoxin. Most VGSCs, termed TTX-sensitive (TTXs), have been both found in brain and sensory neurons where they have a low threshold for activation and rapid inactivation kinetics; by contrast other VGSCs are termed TTX-resistant (TTXr). These may play a key role in persistent pain states, including neuropathic and chronic inflammatory pain.
