Tat-CBD3 (trifluoroacetate salt)

Tat-CBD3 is an inhibitor of the protein-protein interaction between the N-type voltage-gated calcium channel Ca_v2.2 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 Ca_v2.2-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 persensitivity in rats.²