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

M. H. ESTRADA; H. INSUASTY; L. E. CUCA; M. MARDER; A. FIERRO; M. F. GUERRERO

BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES

UNIV SAO PAULO

Lugar: Ribeirao Preto; Año: 2014 vol. 50 p. 73 - 80

1984-8250

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 (IC50: 24.5 ìM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.