Tat-CBD3 (trifluoroacetate salt)

Tat-CBD3 is an inhibitor of the protein-protein interaction between the N-type voltage-gated calcium channel Cav2.2 and collapsin response mediator protein 2 (CRMP2).1,2 It also inhibits the protein-protein interaction between CRMP2 and the NMDA receptor NR2B subunit.3 Tat-CBD3 (10 µM) inhibits the Cav2.2-CRMP2 interaction by 43% in a cell-free assay and the NMDA receptor NR2B subunit-CRMP2 interaction in an immunoprecipitation assay.2,3 It reduces voltage-induced calcium currents by approximately 60% in primary rat dorsal root ganglion (DRG) neurons and glutamate-induced increases in cytosolic calcium levels in primary rat hippocampal neurons.1,3 Tat-CBD3 (20 mg/kg) decreases infarct volume in a rat model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO).4 Intrathecal administration of Tat-CBD3 (20 µg/5 µl) prevents carrageenan-induced thermal hypersensitivity in rats.2WARNING This product is not for human or veterinary use.

[1] JOEL M BRITTAIN. Suppression of inflammatory and neuropathic pain by uncoupling CRMP-2 from the presynaptic Ca2+ channel complex[J]. Nature Medicine, 2011, 17 7: 822-829. DOI: 10.1038/nm.2345
[2] LIBERTY FRANÇOIS-MOUTAL. A membrane-delimited N-myristoylated CRMP2 peptide aptamer inhibits CaV2.2 trafficking and reverses inflammatory and postoperative pain behaviors.[J]. PAIN®, 2015, 156 7: 1247-1264. DOI: 10.1097/j.pain.0000000000000147
[3] TATIANA BRUSTOVETSKY. Collapsin response mediator protein 2 (CRMP2) interacts with N-methyl-D-aspartate (NMDA) receptor and Na+/Ca2+ exchanger and regulates their functional activity.[J]. The Journal of Biological Chemistry, 2014, 289 11: 7470-7482. DOI: 10.1074/jbc.m113.518472
[4] JOEL M BRITTAIN. Disruption of NMDAR-CRMP-2 signaling protects against focal cerebral ischemic damage in the rat middle cerebral artery occlusion model.[J]. Channels (Austin, Tex.), 2012, 6 1: 52-59. DOI: 10.4161/chan.18919