Open Access. Powered by Scholars. Published by Universities.®

Medicine and Health Sciences Commons™

Open Access. Powered by Scholars. Published by Universities.®

Selected Works

Brivaracetam

Articles 1 - 2 of 2

Full-Text Articles in Medicine and Health Sciences

A New Sv2a Ligand For Epilepsy, Michael A. Rogawski Oct 2016

A New Sv2a Ligand For Epilepsy, Michael A. Rogawski

Michael A. Rogawski

Since the 1970s, racetams have been in use as cognitive enhancers. Levetiracetam was discovered to have antiseizure activity in animal models and was then found to bind to SV2A in synaptic and endocrine vesicles. Brivaracetam, an analog of levetiracetam, was identified in a medicinal chemistry campaign with the objective of discovering analogs with higher affinity at racetam-binding sites and greater antiseizure potency.

Go to article

Brivaracetam: A Rational Drug Discovery Success Story, Michael Rogawski Jan 2008

Brivaracetam: A Rational Drug Discovery Success Story, Michael Rogawski

Michael A. Rogawski

Levetiracetam, the alpha-ethyl analogue of the nootropic piracetam, is a widely used antiepileptic drug (AED) that provides protection against partial seizures and is also effective in the treatment of primary generalized seizure syndromes including juvenile myoclonic epilepsy. Levetiracetam was discovered in 1992 through screening in audiogenic seizure susceptible mice and, 3 years later, was reported to exhibit saturable, stereospecific binding in brain to a approximately 90 kDa protein, later identified as the ubiquitous synaptic vesicle glycoprotein SV2A. A large-scale screening effort to optimize binding affinity identified the 4-n-propyl analogue, brivaracetam, as having greater potency and a broadened spectrum of activity …

Go to article