Abstract
We have evaluated as sodium channel blockers a series of imidazobenzoxazines, imidazobenzoxazin-5-ones and imidazobenzoxazin-5-thiones. We tested these new compounds on NaV1.6 and NaV1.2 sodium channel isoforms, that are expressed in central nervous system and seems to be very important in controlling neuronal firing. Moreover, mutations in SCN2A, the gene encoding NaV1.2, have been identified in patients with generalized epilepsy. Almost all of the new molecules were able to block the NaV1.6 sodium currents and some of them displayed IC50 values in the low micromolar range.
Keywords: Antiepileptic drugs, Imidazobenzoxazines, NaV1.6 sodium channel isoforms, Voltage gated sodium channels.
Letters in Drug Design & Discovery
Title:Biological Evaluation of Imidazobenzoxazines, Imidazobenzoxazin-5-ones and Imidazobenzoxazin-5-thiones as Sodium Channel Blockers
Volume: 11 Issue: 1
Author(s): Mirko Rivara, Valentina Zuliani and Manoj K. Patel
Affiliation:
Keywords: Antiepileptic drugs, Imidazobenzoxazines, NaV1.6 sodium channel isoforms, Voltage gated sodium channels.
Abstract: We have evaluated as sodium channel blockers a series of imidazobenzoxazines, imidazobenzoxazin-5-ones and imidazobenzoxazin-5-thiones. We tested these new compounds on NaV1.6 and NaV1.2 sodium channel isoforms, that are expressed in central nervous system and seems to be very important in controlling neuronal firing. Moreover, mutations in SCN2A, the gene encoding NaV1.2, have been identified in patients with generalized epilepsy. Almost all of the new molecules were able to block the NaV1.6 sodium currents and some of them displayed IC50 values in the low micromolar range.
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Cite this article as:
Rivara Mirko, Zuliani Valentina and Patel K. Manoj, Biological Evaluation of Imidazobenzoxazines, Imidazobenzoxazin-5-ones and Imidazobenzoxazin-5-thiones as Sodium Channel Blockers, Letters in Drug Design & Discovery 2014; 11 (1) . https://dx.doi.org/10.2174/15701808113109990050
DOI https://dx.doi.org/10.2174/15701808113109990050 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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