BTT-369 is a Ca V α 1 ·Ca V β 3 protein-protein complex antagonist with a K i of 2.0 μM. BTT-369 inhibits Ca V 2.2 currents, with an apparent IC 50 value of 31 μM. BTT-369 disrupts the interaction between Ca V α 1 and Ca V β 3 subunits. BTT-369 reduces the current density of Ca V 2.2 , and shifts the voltage dependence of steady-state inactivation and activation of Ca V 2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain.
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