Trends in Pharmacological Sciences
Tips reviewCommon modes of drug action on Na+ channels: local anesthetics, antiarrhythmics and anticonvulsants
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Voltage-Gated Sodium Channels and Electrical Excitability of the Heart
2018, Cardiac Electrophysiology: From Cell to Bedside: Seventh EditionA peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats
2014, Biochemical PharmacologyCitation Excerpt :This report describes the in vitro and in vivo pharmacology of a structurally novel and peripherally selective T-type Ca2+ channel blocker, ABT-639 (Fig. 1). The ability of test compounds to block individual Ca2+ channel isoforms (N-type, L-type, P/Q-type and T-type) was determined using previously published ion channel protocols from our laboratories including FLIPR based Ca2+ flux assays, patch clamp electrophysiology, and KCl stimulated aortic strip assays (L-type Ca2+ channels) [20–24]. Recombinant human T-type (Cav3.2) channels stably expressed in HEK293 cells were provided by Dr. Ed Perez-Reyes (University of Virginia, VA).
Voltage-Gated Sodium Channels and Electrical Excitability of the Heart
2014, Cardiac Electrophysiology: From Cell to Bedside: Sixth EditionVoltage-gated sodium channels as insecticide targets
2014, Advances in Insect PhysiologyA highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: Design of potent new ligands
2014, Bioorganic and Medicinal ChemistryCitation Excerpt :To achieve this goal, we proposed to develop a more comprehensive 3-D QSAR model that can include structural information associated with a much greater variety of structural types and drug classes that all bind to the sodium channel. This includes local anesthetics, anticonvulsants, and antiarrhythmics, which have been proposed to bind to the same receptor site.29–34 In the present study we used a training set of 67 sodium channel blockers, 36 of which were synthesized in our laboratory and 31 sodium channel blockers from the literature.35