Tying a GABA from Copenhagen to Chicago The Chemistry of Tiagabine

TYING A GABA FROM COPENHAGEN TO CHICAGO THE CHEMISTRY OF TIAGABINE 

Epilepsy is a disorder characterized by recurrent spontaneous electrical discharges within the brain which are manifested by clinical seizures. Four million patients in the United States are afflicted with this ailment 20% of these have seizures that cannot be controlled sufficiently with existing medications to permit normal activities of everyday life. The market for anticonvulsants is substantial a historical growth rate of 10 to 12% is expected to be sustained thereafter. Epileptic seizures can be classified as primary epilepsies (35%) or partial epilepsies (65%). Primary epilepsies (generalized convulsions) can be controlled with valproate (Depakote), carbamazepine (Tegretol), phenytoin (Dilantin), or phenobarbi-tol. Most partial epilepsies have resisted control with chemotherapeutic agents. 

Drug Discovery and Development, Volume 2 Drug Development, Edited by Mukund S. Chorghade Copyright 2007 John Wiley Sons, Inc. 

Several drugs marketed currently have exhibited problems with toxicity or tetratoge-nicity. Hepatotoxicity, aplastic anemia, Stevens-Johnson syndrome, and neurotoxicity have been concerns cited frequently. Idiosyncratic reactions involving hematologic and dermatologic systems have proved fatal in a few cases. Considerable research effort has been directed toward identifying novel pharmaceutical moieties with a broad spectrum of efficacy and fewer side effects. 

I is the principal inhibitory neurotransmitter in the mammalian central nervous system (CNS). It may inhibit mammahan CNS activity in numerous ways  

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