Local Anesthetic Anchoring to Cardiac Sodium Channels
نویسندگان
چکیده
منابع مشابه
Local anesthetic anchoring to cardiac sodium channels. Implications into tissue-selective drug targeting.
Local anesthetics inhibit Na+ 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 ...
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Effects of flecainide, a potent antiarrhythmic agent, on sodium channel availability was investigated in guinea pig single cardiac cells by the whole-cell voltage-clamp technique. Sodium current (INa) experiments were performed at 170 C, and maximum upstroke velocity (Vmax) experiments were performed at 370 C. Flecainide (3 ,M) caused little tonic block, but reduced sodium channel availability ...
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متن کاملElectrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.
Antiarrhythmics, anticonvulsants, and local anesthetics target voltage-gated sodium channels, decreasing excitability of nerve and muscle cells. Channel inhibition by members of this family of cationic, hydrophobic drugs relies on the presence of highly conserved aromatic residues in the pore-lining S6 segment of the fourth homologous domain of the channel. We tested whether channel inhibition ...
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ژورنال
عنوان ژورنال: Circulation Research
سال: 1999
ISSN: 0009-7330,1524-4571
DOI: 10.1161/01.res.85.1.88