SNX-482

SNX-482, a peptide, is a potent, high affinity, selective and voltage-dependent R-type Ca_V2.3 channel blocker with an IC₅₀ of 30 nM. SNX-482 has antinociceptive effect^[1][2][3]. IC50 & Target:IC50: 30 nM (CaV2.3 channel)^[2] In Vitro:SNX-482 blocks the class E Ca²⁺ channel with an IC₅₀ of 15-30 nM, using either patch clamp electrophysiology or K⁺-evoked Ca²⁺ flux^[1].
At low nanomolar concentrations, SNX-482 also blocks a native resistant or R-type Ca²⁺ current in rat neurohypophyseal nerve terminals, but concentrations of 200-500 nM have no effect on R-type Ca²⁺ currents in several types of rat central neurons^[1].
In Vivo:SNX-482 (0.5-4 μg/5 0μL; applied directly onto the spinal cord; 14-17 days post-operation) in the spinal nerve ligation (SNL) rat model dose - dependently inhibits nociceptive C-fiber and Aδ-fiber-mediated neuronal responses, and the responses to non-noxious mechanical and thermal stimuli are more sensitive in SNL rats than in sham - operated rats^[3].