Solid-form screening of antiepileptic drug retigabine

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چکیده

منابع مشابه

Retigabine: the newer potential antiepileptic drug.

Retigabine represents an antiepileptic drug possessing a completely different mechanism of action when compared to the existing classical and newer antiepileptic drugs. In the therapeutic range, retigabine enhances potassium currents, very likely via destabilization of a closed conformation or stabilization of the open conformation of the potassium Kv7.2-7.3 channels. There are also data indica...

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Solid Dispersion Approach Improving Dissolution Rate of Stiripentol: a Novel Antiepileptic Drug

Some drugs have low bioavailability due to their poor aqueous solubility and/or slowdissolution rate in biological fluids. Stiripentol (STP) is a novel anticonvulsant drug that isstructurally unrelated to the currently available antiepileptics. It has poor aqueous solubilityand its solubility has to be enhanced accordingly. Polyethyleneglycol 6000 (PEG-6000) iscommonly utilized as a hydrophilic...

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[Retigabine - a new antiepileptic drug with a different mechanism of action].

Retigabine belongs to a new generation of antiepileptic drugs. Its mechanism of action is different from that previously known. Retigabine opens potassium channels of subfamily Kv 7, especially Kv 7.2 and Kv 7.3. The drug enhances GABA-ergic transmission. It is well absorbed from the digestive system and undergoes metabolism via glucuronidation and acetylation. There is no interaction between r...

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P-retigabine: an N-propargyled retigabine with improved brain distribution and enhanced antiepileptic activity.

Retigabine (RTG, [ethyl N-[2-amino-4-[(4-fluorophenyl)methyl]amino] phenyl] carbamate]) is a first-in-class antiepileptic drug that acts by potentiating neuronal KCNQ potassium channels; however, it has less than optimal brain distribution. In this study, we report that P-RTG (ethyl N-[2-amino-4-((4-fluorobenzyl)(prop-2-ynyl)amino)phenyl]carbamate), an RTG derivative that incorporates a proparg...

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Solid Dispersion Approach Improving Dissolution Rate of Stiripentol: a Novel Antiepileptic Drug

Some drugs have low bioavailability due to their poor aqueous solubility and/or slowdissolution rate in biological fluids. Stiripentol (STP) is a novel anticonvulsant drug that isstructurally unrelated to the currently available antiepileptics. It has poor aqueous solubilityand its solubility has to be enhanced accordingly. Polyethyleneglycol 6000 (PEG-6000) iscommonly utilized as a hydrophilic...

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ژورنال

عنوان ژورنال: Acta Crystallographica Section A Foundations and Advances

سال: 2017

ISSN: 2053-2733

DOI: 10.1107/s2053273317088155