Uses
SNX-482, a peptide, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect[1][2][3].
Biological Activity
SNX-482 is a peptidyl toxin originally isolated from the venom of the spider Hysterocrates gigas. SNX-482 specifically blocks Cav2.3 (a1E, R-type) calcium channels in a voltage dependent manner. SNX-482 also blocks P/Q-type voltage-gated Ca2+ channels and blocks A-type K+ channels (IC50 of <3 nm).
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].
| Animal Model: | Male Sprague-Dawley rats (initially weighing 130-150 g) + Spinal nerve ligation[3] |
| Dosage: | 0.5 μg/50 μL, 1.5 μg/50 μL, 4 μg/50 μL |
| Administration: | Applied directly onto the spinal cord, 14-17 days post-operation |
| Result: | Exerted a significant dose-related inhibitory effect on C-fiber evoked responses, Aδ-fiber responses, post-discharge and input measurements.
Inhibited the "wind-up" of neurons. |
storage
-20°C (desiccate)
References
[1] R Newcomb, et al. Selective peptide antagonist of the class E calcium channel from the venom of the tarantula Hysterocrates gigas. Biochemistry. 1998 Nov 3;37(44):15353-62. DOI:
10.1021/bi981255g[2] E Bourinet, et al. Interaction of SNX482 with domains III and IV inhibits activation gating of alpha(1E) (Ca(V)2.3) calcium channels. Biophys J. 2001 Jul;81(1):79-88. DOI:
10.1016/S0006-3495(01)75681-0[3] Elizabeth A Matthews, et al. The Cav2.3 calcium channel antagonist SNX-482 reduces dorsal horn neuronal responses in a rat model of chronic neuropathic pain. Eur J Neurosci. 2007 Jun;25(12):3561-9. DOI:
10.1111/j.1460-9568.2007.05605.x
