کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2563402 1127527 2010 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Neuronal and non-neuronal GABA transporters as targets for antiepileptic drugs
کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی داروشناسی
پیش نمایش صفحه اول مقاله
Neuronal and non-neuronal GABA transporters as targets for antiepileptic drugs
چکیده انگلیسی

Epileptic seizure activity is associated with an imbalance between excitatory and inhibitory synaptic activities. The latter is mediated by GABA, and several currently used antiepileptic drugs target entities of the GABAergic synapse such as the receptors or the inactivation mechanism consisting of transmembrane transport and enzymatic degradation. The development of tiagabine selectively inhibiting the GABA transporter GAT1 constitutes a proof of concept that the GABA transporters are interesting drug targets in the context of antiepileptic drugs. The review provides a detailed analysis of the role of such transporters pointing in particular to an interesting role of the transporters located extrasynaptically. It is suggested that the betaine–GABA transporter BGT1 should receive particular interest in this context as the GABA analogue EF 1502 (N-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-4-(methylamino)-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol) has been shown to possess a novel anticonvulsant profile in animal models of epilepsy, involving the ability to inhibit GABA transport mediated by GAT1 and BGT1 at the same time.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacology & Therapeutics - Volume 125, Issue 3, March 2010, Pages 394–401
نویسندگان
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