Anticonvulsants

Abstract

This chapter focuses on the chemical structures, the mechanism of action and the main structure–activity relationships of selected current and prospective anticonvulsant agents. Particular attention will be addressed to molecular targets involved in the mechanism of action of not only currently used drugs but also now being developed drugs. The pharmacokinetic and pharmacodynamic aspects of the most representative anticonvulsant agents will be also considered.

The Positive Allosteric Modulator ofα2/3-Containing GABAAReceptors, KRM-II-81, Is Active in Pharmaco-Resistant Models of Epilepsy and Reduces Hyperexcitability after Traumatic Brain Injury

“…The need for new antiepileptic drugs continues to be high despite the availability of a host of marketed drugs of different mechanistic classes (Gitto et al, 2010). The lack of seizure control in patients is the primary factor driving this demand (Sinha and Siddiqui, 2011).…”

“…The lack of seizure control in patients is the primary factor driving this demand (Sinha and Siddiqui, 2011). Increasing inhibitory tone in the central nervous system through enhancement of GABAergic inhibition is a proven mechanism for seizure control (Gitto et al, 2010). However, GABAergic medications also exhibit some liabilities that limit their antiepileptic potential.…”

“…Although enhancing GABAergic inhibitory tone is a wellestablished mechanism for seizure protection with multiple anticonvulsant drugs approved in this class (White et al, 2007;Gitto et al, 2010), recent attention has been directed toward GABA modulators that have reduced side-effect liabilities. In particular, the potential advantages of developing positive allosteric modulators (PAMs) of a2/3-containing GABA A receptors as antiepileptic drugs has come to the forefront in the last 2 years.…”

N-Chlorination rate of five-membered heterocyclic nitrogen compounds

“…This set of heterocyclic organic compounds of five atoms (Fig. ) and their derivatives, very different chemically but with similar structures, is very interesting from the point of view pharmacologically because of their activity like antiepileptic and anticonvulsants . It is interesting to indicate that the type of substituent at C(5) appears to be extremely important in determining the physiological properties of these compounds…”

“…1) and their derivatives, very different chemically but with similar structures, is very interesting from the point of view pharmacologically because of their activity like antiepileptic and anticonvulsants. [4][5][6][7][8][9] It is interesting to indicate that the type of substituent at C(5) appears to be extremely important in determining the physiological properties of these compounds. [10] Moreover, these heterocyclic compounds and their derivatives are of great interest because they possess other interesting characteristics.…”