Differences in local anaesthetic and antiepileptic binding in the inactivated state of human sodium channel Nav1.4.

ABSTRACT: Voltage-gated sodium channels play a vital role in nerve and muscle cells, enabling them to encode and transmit electrical signals. Currently, there exist several classes of drugs that aim to inhibit these channels for therapeutic purposes, including local anesthetics, antiepileptics and antiarrhythmics. However, sodium-channel-inhibiting drugs lack subtype specificity; instead, they inhibit all sodium channels in the human body. Improving understanding of the mechanisms of binding of existing nonselective drugs is important in providing insight into how subtype-selective drugs could be developed. This study used molecular dynamics simulations to investigate the binding of the antiepileptics carbamazepine and lamotrigine and the local anesthetic lidocaine in neutral and charged states to t

SUBMITTER: Buyan A 

PROVIDER: S-EPMC8715241 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature