Abstract
The glutamate receptor system is implicated in the development and maintenance of epileptic seizures, and animal studies have disclosed potent anticonvulsant activity of a number of inhibitors of AMPA and / or kainate (KA) receptor activity. These results make such inhibitors potential future antiepileptic drugs. Different series of compounds with inhibitory activity towards AMPA receptors have been developed. Most of these inhibitors are structurally derived from AMPA, quinoxalinedione or 2,3-benzodiazepine. In contrast, only a limited number of inhibitors of KA receptor activity have been developed, most of which contain quinoxalinedione or decahydroisoquinoline skeletons. In spite of promising anticonvulsant activity in various animal model studies, no AMPA / KA receptor inhibitors are in clinical use against epilepsy today. Based on molecular biology studies, AMPA and KA receptors are at present divided into four and five subtypes, respectively, and attempts to develop subtype selective compounds have been initiated. Future studies and development of such compounds will indicate whether AMPA / KA receptor inhibition is a feasible therapeutic strategy for the treatment of epilepsy.
Keywords: ampa, kainate rexeptors, n-methyl-d-aspartate nmda, amino hydroxy methyl isoxazolyl propionate amp, ampa receptor agonists, ampa receptor antagonists, anticonvulsant actvity, ka receptor agonists
Current Medicinal Chemistry
Title: Inhibitors of AMPA and Kainate Receptors
Volume: 8 Issue: 11
Author(s): U. Madsen, T. B. Stensbol and P. Krogsgaard-Larsen
Affiliation:
Keywords: ampa, kainate rexeptors, n-methyl-d-aspartate nmda, amino hydroxy methyl isoxazolyl propionate amp, ampa receptor agonists, ampa receptor antagonists, anticonvulsant actvity, ka receptor agonists
Abstract: The glutamate receptor system is implicated in the development and maintenance of epileptic seizures, and animal studies have disclosed potent anticonvulsant activity of a number of inhibitors of AMPA and / or kainate (KA) receptor activity. These results make such inhibitors potential future antiepileptic drugs. Different series of compounds with inhibitory activity towards AMPA receptors have been developed. Most of these inhibitors are structurally derived from AMPA, quinoxalinedione or 2,3-benzodiazepine. In contrast, only a limited number of inhibitors of KA receptor activity have been developed, most of which contain quinoxalinedione or decahydroisoquinoline skeletons. In spite of promising anticonvulsant activity in various animal model studies, no AMPA / KA receptor inhibitors are in clinical use against epilepsy today. Based on molecular biology studies, AMPA and KA receptors are at present divided into four and five subtypes, respectively, and attempts to develop subtype selective compounds have been initiated. Future studies and development of such compounds will indicate whether AMPA / KA receptor inhibition is a feasible therapeutic strategy for the treatment of epilepsy.
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Cite this article as:
Madsen U., Stensbol B. T. and Krogsgaard-Larsen P., Inhibitors of AMPA and Kainate Receptors, Current Medicinal Chemistry 2001; 8 (11) . https://dx.doi.org/10.2174/0929867013372210
DOI https://dx.doi.org/10.2174/0929867013372210 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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