BTT-369

BTT-369 is a Ca_Vα₁·Ca_Vβ₃ protein-protein complex antagonist with a K_i of 2.0 μM. BTT-369 inhibits Ca_V2.2 currents, with an apparent IC₅₀ value of 31 μM. BTT-369 disrupts the interaction between Ca_Vα₁ and Ca_Vβ₃ subunits. BTT-369 reduces the current density of Ca_V2.2, and shifts the voltage dependence of steady-state inactivation and activation of Ca_V2.2 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^[1]. In Vitro:BTT-369 potently inhibits the protein-protein interaction between purified Ca_Vα₁-AID and Ca_Vβ₃, with a K_i value of 2.0 μM^[1].
BTT-369 (0.1-100 μM; 5 min-48 h) reduces Ca_V2.2 current density in HEK-CaV2.2 cells, and shifts the voltage dependence of Ca_V2.2 activation and steady-state inactivation toward more positive potentials^[1]. In Vivo:BTT-369 (0.1 mg/kg; i.p.; single bolus injection) significantly reverses mechanical hypersensitivity in a rat tibial nerve injury model of neuropathic pain for at least 24 hours^[1].