PERAMPANEL activity on Epileptiform Discharges

PERAMPANEL activity on Epileptiform Discharges

Most of the anti-epileptic drugs (AED) have been developed empirically and have multiple targets, multiple mechanisms of actions, and sometime multiple side effects. Now let’s look at PERAMPANEL.

Evolution of anti-epileptic drugs

For the past couple of years, pharmaceutical and biotech companies have been trying to develop new AED based on a single target and mechanism of action, for a better control of efficacy and of potential  side effects. In addition, epilepsies are of diverse origins and with many different neuropathological profiles and they must be addressed individually. There is no way for a “magic pill” that could treat all kinds of epilepsies.

PERAMPANEL is a new first in class AED

PERAMPANEL is a new – first-in-class – antiepileptic drug (Fycompa™, by EISAI). This new molecule is a highly-selective non-competitive antagonist of AMPA receptors, with no action on the other glutamate receptors. It is the first antiepileptic drug blocking the AMPA receptors function, which are implicated in fast synaptic transmission mediated by glutamate. The pharmacological activity of PERAMPANEL could be illustrated in vitro by titrating its pharmacological activity on Epileptiform Discharges elicited by 4-Amino-Pyridin (4-AP) in rat hippocampal slices recorded with Multi-Electrode Arrays.

perampanel

A concentration of 1 µM PERAMPANEL is able to completely inhibit the 4-AP-induced Epileptiform Discharges, as illustrated in the figure. Such protocol has been used by NEUROSERVICE to compare the activity of many anti-epileptic drugs such as Carbamazepine, Phenobarbital, Midazolam, Phenytoin, Lamotrigine, Levetiracetam, Valproate, Gabapentin, Topiramate, and Tiagabine. For more information please contact us at contact@neuroservice.com

About Neuroservice

NEUROSERVICE is a CRO providing functional pharmacological assays performed on acute brain and spinal cord slices. Our mission is to support our customers lead selection and optimization for CNS diseases & PAIN R&D programs. NEUROSERVICE has unparalleled expertise in electrophysiological-based assays performed with the Multi-electrode array (MEA) and Patch-clamp techniques.

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