Epilepsy receptors

Benzodiazepines. Several BZs have anticonvulsant activity and ate used for the treatment of epilepsy producing their anticonvulsant actions via interactions with the GABA /BZ receptor complex to enhance inhibitory GABAergic transmission (1). The anticonvulsant actions of the BZs tend to tolerate upon chronic usage in six months, and BZs also lead to withdrawal symptomatology. Other side effects include sedation, ataxia, and cognitive impairment. 

Altered synaptic properties Numerous changes in the properties of inhibitory (GABAergic) and excitatory (glutamatergic) synapses have been reported. While the simple adage of an imbalance between inhibitory and excitatory neurotransmission in epilepsy is not generally applicable, some forms of inhibition are lost or impaired in epilepsy. Likewise, an increased function of glutamate receptors has been demonstrated in some brain areas. 

On the basis of the events that occur in pain and LTP, it is easy to see how the actions of glutamate relate to the excessive firing of neurons — as yet no NMDA receptor antagonist has been tested in human epilepsy. 

Stelzer, A, Slater, NT and Bruggencate, G (1987) Activation of NMD A receptors blocks GABA ergic innervation in an in vitro model of epilepsy. Nature 326 698-701. 

Birioukova LM, Midzyanovskaya IS, Lensu S, Tuomisto L, van Luijtelaar G. Distribution of Di-like and D2-like dopamine receptors in the brain of genetic epileptic WAG/Rij rats. Epilepsy Res 2005 63 89-96. 

Risa J, Risa A, Adsersen A, et al. Screening of plants used in southern Africa for epilepsy and convulsions in the GABAA-benzodiazepine receptor assay. J Ethnophar-macol 2004 93 177-182. 

Drugs that act on the H3 receptor are being developed for treating obesity, sleep disturbances, epilepsy and cognitive disorders 262... 

Drugs that act on the H3 receptor are being developed for the treatment of obesity, sleep disturbances, epilepsy and cognitive disorders. The ability of histamine to promote arousal, suppress appetite, elevate seizure threshold and stimulate cognitive processes implies that compounds able to enhance the release of neuronal histamine should mimic these effects. Several H3 antagonists currently in development demonstrate such activity and show promise as effective and novel therapeutic agents [40, 84-86]. Because H3 agonists suppress the release of... 

The epilepsies constitute a common, serious neurological disorder in humans, affecting approximately 60 million people worldwide. Well in excess of 40 distinct epileptic syndromes have been identified to date. Current treatment is only symptomatic except in uncommon instances when surgical treatment is possible. While available antiseizure medications target ion channels such as the y-amino-butyric acid (GABA)a receptor and voltage activated sodium (Na+) channels, current research seeks to elucidate the cellular and molecular mechanisms by which a normal brain becomes epileptic. Hopefully, this research will lead to the identification of new targets for which small molecules can be identified and used for prevention or cure of epilepsy. 

Gibbs J. W. III, Shumate, M. D. and Coulter, D. A. Differential epilepsy-associated alterations in postsynaptic GABAa receptor function in dentate granule and CA1 neurons. J. Neurophysiol. 77 1924-1938,1997. 

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