Pharmacokinetics and pharmacodynamics of safinamide, a neuroprotectant with antiparkinsonian and anticonvulsant activity

Marzo, A; Bo, Lorenzo Dal; Monti, N.; Crivelli, Fabrizio; Ismaili, Shevqet; Caccia, C.; Cattaneo, C; Fariello, Ruggero G.

doi:10.1016/j.phrs.2003.12.004

Cited by 102 publications

(116 citation statements)

References 8 publications

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“…Hence, it becomes necessary to determine the bioavailability of the tested chemicals. In the present study, we calculated the maximum concentration (C max ) test species is actually exposed (Marzo et al 2004). This could help us in determining an approximate value for both bioavailability and effective range of a particular chemical to the test organism, as pointed by Saghir et al (2006).…”

Section: Edc Toxicity On C Polykrikoidesmentioning

confidence: 99%

Evaluation of the sub-lethal toxicity of Cu, Pb, bisphenol A and polychlorinated biphenyl to the marine dinoflagellate Cochlodinium polykrikoides

Ebenezer¹,

2012

ALGAE

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Algae are sensitive to a wide range of pollutants, and are effective bioindicators in ecotoxicity assessments. Here, we evaluated the sub-lethal sensitivity of the marine dinoflagellate Cochlodinium polykrikoides upon exposure to copper (Cu), lead (Pb), bisphenol A (BPA), and Aroclor 1016 (polychlorinated biphenyl, PCB). Toxic effects were assessed by observations of the reduction in cell counts and chlorophyll a levels after exposure to each toxicant. C. polykrikoides displayed dose-dependent, sigmoidal responses when exposed to the tested chemicals. EC 50 -72 h values for Cu, Pb, BPA, and PCB were 12.74, 46.70, 68.15, and 1.07 mg L -1 , respectively. PCB, which is an endocrine-disrupting chemical, was the most sensitive, proving its toxic effect on the dinoflagellate. This study provides baseline data on the toxic effects of commonly used heavy metals and endocrine-disrupting chemicals to a marine dinoflagellate.

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Section: Edc Toxicity On C Polykrikoidesmentioning

confidence: 99%

Evaluation of the sub-lethal toxicity of Cu, Pb, bisphenol A and polychlorinated biphenyl to the marine dinoflagellate Cochlodinium polykrikoides

Ebenezer¹,

2012

ALGAE

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“…Chemically, Safinamide is (S)-(+)-2-[4-(3-fluorobenzyloxybenzylamino) propanamide] methane sulfonate (1 : 1 salt) ( Figure 1) [1,2].…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of HPTLC Method for Estimation of Safinamide Mesylate in Bulk and in Tablet Dosage Form

Redasani

Mali

Surana

2012

ISRN Analytical Chemistry

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A simple, specific, and precise high-performance thin-layer chromatographic method has been developed and validated for estimation of Safinamide Mesylate as bulk and in tablet dosage form. The chromatographic development was carried out on aluminum plates precoated with silica gel 60 F254 using a mixture of Toluene: Methanol: Triethylamine (4 : 1 : 0.5 v/v) as mobile phase. Detection was carried out densitometrically at 226 nm. The R F value of drug was found to be 0.54 ± 0.02. The method was validated with respect to linearity, accuracy, precision, and robustness. The calibration curve was found to be linear over a range of 400-2400 ng μL −1 . The % assay (Mean ± S.D.) was found to be 100.27 ± 0.72. Accuracy of the method was accessed by percentage recovery and found to be 99.77±0.71%. Thus the proposed HPTLC method was found to provide fast and cost-effective quantitative control for routine analysis of Safinamide mesylate as bulk and in tablet dosage form.

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“…Some anticonvulsants like lamotrigine and zonizamide are effective against MES, preventing tonic clonic seizures in man and displaying inhibitory effects against MAO-B (Muck-Seler et al, 2008;Sonsalla et al, 2010). This property suggests a neuroprotective effect due to a reduction in reactive oxygen species generated in the central nervous system by this enzyme, a characteristic that could be of special interest in searching for modern anticonvulsant drugs (Marzo et al, 2004). MAO inhibition has been described as a possible anticonvulsant mechanism of action of some agents.…”

Section: Discussionmentioning

confidence: 99%

Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine

Estrada

Insuasty

Suárez

et al. 2014

Braz. J. Pharm. Sci.

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This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo [1,5-a] [1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC 50 : 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition. Unitermos: Pirazol-triazina/perfil anticonvulsivante. Anticonvulsivantes/estudo experimental. Monoaminoxidase/inibidores.

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Pharmacokinetics and pharmacodynamics of safinamide, a neuroprotectant with antiparkinsonian and anticonvulsant activity

Cited by 102 publications

References 8 publications

Evaluation of the sub-lethal toxicity of Cu, Pb, bisphenol A and polychlorinated biphenyl to the marine dinoflagellate Cochlodinium polykrikoides

Evaluation of the sub-lethal toxicity of Cu, Pb, bisphenol A and polychlorinated biphenyl to the marine dinoflagellate Cochlodinium polykrikoides

Development and Validation of HPTLC Method for Estimation of Safinamide Mesylate in Bulk and in Tablet Dosage Form

Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine

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