Get Antiepileptic Drug Discovery: Novel Approaches PDF


By Alan Talevi, Luisa Rocha

ISBN-10: 1493963538

ISBN-13: 9781493963539

ISBN-10: 1493963554

ISBN-13: 9781493963553

This thorough quantity delves into antiepileptic drug discovery with a entire choice of cutting edge methods for the advance of antiepileptic remedies, concentrating on novel molecular ambitions for antiepileptic medications, computer-aided ways for the identity of latest drug applicants, and healing recommendations to beat refractory epilepsy. The final part illustrates the aptitude merits that community pharmacology and rational drug repurposing may well convey to the antiepileptic drug discovery neighborhood. Written for the Methods in Pharmacology and Toxicology sequence, chapters contain the type of specific description and implementation recommendation to make sure ends up in the laboratory.
Authoritative and useful, Antiepileptic Drug Discovery: Novel Approaches goals to supply medicinal chemists, pharmacologists, and different researchers with the instruments have to extra discover the learn of pharmacoresistant epilepsy and the invention of recent antiepileptic drugs.

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Brain 138:1208–1222 14. Khalil M, Ronda J, Weintraub M et al (2007) Brain mast cell relationship to neurovasculature during development. Brain Res 1171: 18–29 15. Zhuang X, Silverman AJ, Silver R (1996) Brain mast cell degranulation regulates blood-brain barrier. J Neurobiol 31(4):393–403 16. Cocchiara R, Albeggiani G, Lampiasi N (1999) Histamine and tumor necrosis factor-alpha production from purified rat brain mast cells mediated by substance P. Neuroreport 10(3): 575–578 17. Jin Y, Silverman AJ, Vannucci SJ (2009) Mast cells are early responders after hypoxia-ischemia in immature rat brain.

The pH is mainly balanced by the buffer CO2/HCO3− (in the intracellular and extracellular space), so several links between CAs and the generation of seizures have been proposed [11]. Furthermore, the relation of CA and seizures is supported by the fact that CA inhibitors are (or were) employed to treat epilepsy. For example, in 1963, Esplin and Rosertain studied the inhibitor acetazolamide and they found that it decreased excitability in cat spinal cord [24]. After that, other authors proposed that the glial cells are more alkaline than neurons (due to higher concentrations of HCO3−), and the anticonvulsant action of the CA inhibitors could be related with extracellular acidosis [25].

2). The most important functional group that serves as Zn2+ anchoring group of CA inhibitors is the sulfonamide function (and their bioisosteric partners, Fig. 2). However, it is worth pointing out that other inhibition mechanisms have been discovered for other families of compounds, such as polyamines and coumarins [12]. Some commercial AEDs are CA inhibitors [29]. However, their anticonvulsant action has not been totally attributed to the CA inhibition process in most of the compounds. In fact, the CA interactions represent a drug weakness in some cases, because it generates tolerance and/or important side effects.

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Antiepileptic Drug Discovery: Novel Approaches by Alan Talevi, Luisa Rocha

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