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8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects BJPS
Olaya,María del Pilar; Vergel,Nadezdha Esperanza; López,Jose Luis; Viña,Dolores; Guerrero,Mario Francisco.
Parkinson’s disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson’s disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Parkinson’s disease; Monoamine oxidase B; Coumarin; Mice; Reserpine; Levodopa; Carbidopa.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100508
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Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine BJPS
Estrada,Martín Hermógenes; Insuasty,Henry; Cuca,Luis Enrique; Marder,Mariel; Fierro,Angélica; Guerrero,Mario Francisco.
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.)...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Pyrazolo-triazine/anticonvulsant profile; Anticonvulsants/experimental study; Monoamine oxidase/inhibitors.
Ano: 2014 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502014000100007
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Croton schiedeanus Schltd prevents experimental hypertension in rats induced by nitric oxide deficit BJPS
Páez,María Teresa; Rodríguez,Diana Catalina; López,Daniel Fernando; Castañeda,Jorge Arturo; Buitrago,Diana Marcela; Cuca,Luis Enrique; Guerrero,Mario Francisco.
Croton schiedeanus Schltd (N.V.: "almizclillo") is a plant used in traditional medicine as an antihypertensive in Colombia. It contains flavonoid, diterpenoid and fenilbutanoid metabolites that have vasodilatation effects linked to the NO/cGMP pathway. This work aimed to assess the capacity of a 96% EtOH extract to prevent the hypertension induced by nitric oxide (NO) deficiency in rats. The NO synthase inhibitor L-NAME (10 mg/kg/d, i.p) was administered during five weeks to three groups of rats (6-7 animals): C. Schiedeanus (200 mg/kg/d, p.o), enalapril (reference, 10 mg/kg/d, p.o) and vehicle (control: olive oil 1 ml/kg/d, p.o). In addition, the blank group received only vehicle. The arterial blood pressure (BP) and heart rate (HR) were measured daily...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Croton schiedeanus/pharmacognosy; Almizelillo/use; Almizelillo/hypertension prevention; Nitric oxide/deficit; Hypertension/prevention; Plant extracts/vasodilatation effects; Medicinal plants.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000400027
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