Hydantoins

Jones, Gary L.; Wimbish, Gary H.

doi:10.1007/978-3-642-69518-6_13

Cited by 11 publications

(2 citation statements)

References 182 publications

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“…They can decrease resting fluxes of Na + as well as Na + currents that flow during action potentials or chemically induced depolarization (18). The latter effects probably result from inhibition of voltage-sensitive Na + channels.…”

Section: Mechanism Of Actionmentioning

confidence: 99%

Clinical and Pharmaceutical Applications of Gas Chromatography

Álvarez

2004

Modern Practice of Gas Chromatography

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Section: Mechanism Of Actionmentioning

confidence: 99%

Clinical and Pharmaceutical Applications of Gas Chromatography

Álvarez

2004

Modern Practice of Gas Chromatography

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“…Immense AEDs, hailing from different groups, are commonly used to control seizures, like phenytoin, carbamazepine, valproic acid, topiramate, gabapentin, felbamate, levetiracetam, etc. 6 A significant percentage of epileptic patients have acceptable AED enhancements, but they represent drawbacks such as insufficient seizure regulation, unpredictability of affect and failure, low effectiveness, inadequate knowledge on drug receptors, etc. and the most important downside is the possibility of drug resistance.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Anticonvulsant Evaluation of 3-(5-(4-substitutedphenyl)-4,5-dihydro-1H-pyrazol- 3-ylamino)-2-(2-methylphenyl)quinazolin-4(3H)-one Derivatives

Kumar¹,

Jha²,

Tripathi³

et al. 2021

IJPER

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Epilepsy arise due to discharge of electric current in CNS and it is Characterized by repeated seizure because of different factors like social, neurological and environmental or it may be due to genetic or non-genetic. A large number of AED's used to treat epilepsy but all these shows drug resistance and side effects, so research interest continue to find out novel antiepileptic drugs with higher efficiency and less toxicity.A novel series of 3-(5-(4-substitutedphenyl)-4,5-dihydro-1H-pyrazole-3-ylamino)-2-(2-methylphenyl) quinazole4(3H)-one was developed, synthesized and evaluated for anticonvulsant activity using two pharmacological models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) models. Spectral data and elemental analysis were used to validate the structure of the synthetic compounds. Synthesized substances have also been tested for their neurotoxicity by rotary apparatus. Both compounds display strong anticonvulsant and neurotoxic activity. 3-(5-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-3-ylamino)-2-(2-methylphenyl)quinazole-4(3H)-one, 8(v) was found to be the most successful in maximal electroshock seizure (percentage protection = 73.63 at 150 mg/kg) and subcutaneous pentylenetetrazole induced convulsion model (percentage protection = 75.59 at 150 mg/kg) models and was found to be non-neurotoxic.

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Effect of phenytoin on cytochrome P450 2B mRNA expression in primary rat astrocyte cultures

et al. 1998

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Studies on cytochrome P450 2B (CYP2B) in the brain have essentially been focused on protein characterization and regional distribution. Due to the high sequence homology between the closely related CYP2B1 and 2B2 isoforms and the low amounts of the corresponding mRNAs few efforts have been made to analyze the expression, regulation, and inducibility of these P450 genes in a specific cell type. In the present study, we investigated CYP2B mRNA expression in primary rat astrocyte cultures under the influence of the anti-epileptic drug phenytoin, which is known to be a CYP2B inducing agent in liver. In situ hybridization with a digoxigenin (DIG)-labeled cRNA probe demonstrated that 30-40% of the astrocytes strongly expressed a CYP2B mRNA-specific signal within the first week of cultivation. With increasing age (> 14 days) a greater percentage of cells (>90%) expressed mRNA for P450 2B. However, the level of transcriptional activity was substantially lower than in younger cultures. To discriminate between the 2B1 and 2B2 isoforms the reverse transcription/polymerase chain reaction (RT/PCR) procedures were proved for rat hepatic mRNA as a control assay. Subsequently, the application of this method on cultured astrocytes confirmed that these brain cells may express CYP2B1 mRNA. CYP2B2 mRNA could not be detected in astrocyte cultures at any age examined. Phenytoin led to the down regulation of CYP2B1 mRNA, which contrasts with the drug inducing effect on hepatic CYP2B1 and 2B2 levels. After 4 hr of exposure of phenytoin to the astrocytes no amplification product could be detected at all. Phenytoin did not induce either CYP2B1 or 2B2 expression.

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Hydantoins

Cited by 11 publications

References 182 publications

Clinical and Pharmaceutical Applications of Gas Chromatography

Clinical and Pharmaceutical Applications of Gas Chromatography

Synthesis and Anticonvulsant Evaluation of 3-(5-(4-substitutedphenyl)-4,5-dihydro-1H-pyrazol- 3-ylamino)-2-(2-methylphenyl)quinazolin-4(3H)-one Derivatives

Effect of phenytoin on cytochrome P450 2B mRNA expression in primary rat astrocyte cultures

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