[CAS NO. 94-09-7]  Benzocaine

Benzocaine blocks μ1 wild-type Na ⁺ currents in a dose-dependent Manner. The Benzocaine concentration that inhibits 50% of Na ⁺ currents (IC ₅₀ ) is estimated to be about 0.8 mM when a test potential of +30 mV is applied. The slope of the h∞ curve is also significantly reduced by benzocaine (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about 55% of wild-type Na ⁺ current but about 95% of μ1-N1584A mutant current. Benzocaine also appears to bind more strongly to its LA receptor in the N1584A mutant than in the wild type ^[1] . The inhibition of Ca ²⁺ uptake occurres at lower Benzocaine concentration (IC ₅₀ =40.3±1.2mM) than that affecting the enzymatic activity ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.