PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 34992539-3 2021 It has been reported that lacosamide"s effect on NaV1.5 is sensitive to a mutation in the local anesthetic binding site, and that it binds with slow kinetics to the fast-inactivated state of NaV1.7. Lacosamide 26-36 sodium voltage-gated channel alpha subunit 5 Homo sapiens 49-55 24563546-11 2014 Unexpectedly, lacosamide elicited a time-dependent block of persistent hNav1.5-CW Na(+) currents with an IC50 of 242 +- 19 microM (n = 5). Lacosamide 14-24 sodium voltage-gated channel alpha subunit 5 Homo sapiens 71-78 24563546-12 2014 Furthermore, both hNav1.5-CW/F1760K mutant and batrachotoxin-activated hNav1.5 Na(+) channels became completely lacosamide resistant, indicating that the lacosamide receptor overlaps receptors for local anesthetics and batrachotoxin. Lacosamide 112-122 sodium voltage-gated channel alpha subunit 5 Homo sapiens 18-25 24563546-12 2014 Furthermore, both hNav1.5-CW/F1760K mutant and batrachotoxin-activated hNav1.5 Na(+) channels became completely lacosamide resistant, indicating that the lacosamide receptor overlaps receptors for local anesthetics and batrachotoxin. Lacosamide 112-122 sodium voltage-gated channel alpha subunit 5 Homo sapiens 71-78 24563546-13 2014 Our results together suggest that lacosamide targets the intermediate preopen and open states of hNav1.5 Na(+) channels. Lacosamide 34-44 sodium voltage-gated channel alpha subunit 5 Homo sapiens 97-104 24563546-14 2014 Lacosamide may thus track closely the conformational changes at the hNav1.5-F1760 region along the activation pathway. Lacosamide 0-10 sodium voltage-gated channel alpha subunit 5 Homo sapiens 68-75