Article
The Novel Activity of Carbamazepine as an Activation Modulator Extends from NaV1.7 Mutations to the NaV1.8-S242T Mutant Channel from a Patient with Painful Diabetic Neuropathy.
Molecular pharmacology - 1 Nov 2018
Han Chongyang, Themistocleous Andreas C, Estacion Mark, Dib-Hajj Fadia B, Blesneac Iulia, Macala Lawrence, Fratter Carl, Bennett David L, Waxman Stephen G, Dib-Hajj Sulayman D
Abstract excerpt
Neuropathic pain in patients carrying sodium channel gain-of-function mutations is generally refractory to pharmacotherapy. However, we have shown that pretreatment of cells with clinically achievable concentration of carbamazepine (CBZ; 30 μM) depolarizes the voltage dependence of activation in some NaV1.7 mutations such as S241T, a novel CBZ mode of action of this drug. CBZ reduces the excitability of dorsal...
Topics
- Aged
- Animals
- Carbamazepine
- Diabetic Neuropathies
- Female
- Ganglia, Spinal
- Humans
- Male
- Membrane Potentials
- Mice