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Local Anesthetic Anchoring to Cardiac Sodium Channels : Implications Into Tissue-Selective Drug Targeting
Local anesthetics inhibit Na ϩ channels in a variety of tissues, leading to potentially serious side effects when used clinically. We have created a series of novel local anesthetics by connecting benzocaine (BZ) to the sulfhydryl-reactive group methanethiosulfonate (MTS) via variable-length polyethylether linkers (L) (MTS-LX-BZ [X represents 0, 3, 6, or 9]). The application of MTS-LX-BZ agents modified native rat cardiac as well as heterologously expressed human heart (hH1) and rat skeletaldoi:10.1161/01.res.85.1.88 pmid:10400914 fatcat:se7zzqeuyvcgxmzxhk36lesig4