Voltagegated Sodium Channels

Voltage-gated sodium channels (VGSCs) in the presynaptic nerve terminal of the excitatory glutamate receptors are the molecular target for phenytoin, CBZ, and lamotrigine as well as some of the newer AEDs, such as OXC, felbamate (FBM), and zonisamide.18 These aromatic AEDs inhibit excessive neuronal firing by binding to a site near the inactiva-tion gate, thereby prolonging inactivation of VGSCs.20 Figure 14.1 illustrates how phenytoin interacts with the hypothetical inactivation gate receptor according to a pharmacophore model suggested by Unverferth et al.21 as a result of molecular simulations with these aromatic AEDs. This model includes an aromatic binding site and two separate hydrogen bonding sites for interacting with potent AEDs such as phenytoin and lamotrigine.

Was this article helpful?

0 0
Diabetes 2

Diabetes 2

Diabetes is a disease that affects the way your body uses food. Normally, your body converts sugars, starches and other foods into a form of sugar called glucose. Your body uses glucose for fuel. The cells receive the glucose through the bloodstream. They then use insulin a hormone made by the pancreas to absorb the glucose, convert it into energy, and either use it or store it for later use. Learn more...

Get My Free Ebook


Post a comment