IFLYSIB   05383
INSTITUTO DE FISICA DE LIQUIDOS Y SISTEMAS BIOLOGICOS
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
ANTICONVULSANT SULFAMIDES WITH AFFINITY FOR THE GABAA RECEPTOR AND ANXIOLYTIC
Autor/es:
WASOWSKI C.A, GAVERNET L.B, BARRIOS I.A.B, BRUNO-BLANCH L.E.B, MARDER M.A
Lugar:
Rosario, Argentina
Reunión:
Congreso; Cuadragésima primera REUNION ANUAL de SAFE; 2009
Resumen:
ANTICONVULSANT SULFAMIDES WITH AFFINITY FOR THE GABAA RECEPTOR AND ANXIOLYTIC
ACTIVITY IN MICE.A RECEPTOR AND ANXIOLYTIC
ACTIVITY IN MICE..
Wasowski C.a, Gavernet L.b, Barrios I.A.b, Bruno-Blanch L.E.b, Marder M.a
a IQUIFIB (UBA-CONICET), Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina.a, Gavernet L.b, Barrios I.A.b, Bruno-Blanch L.E.b, Marder M.a
a IQUIFIB (UBA-CONICET), Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina.IQUIFIB (UBA-CONICET), Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina.
b Química Medicinal, Departamento de Ciencias Biológicas, UNLP, calle 47 y 115 (B1900BJW), La Plata, Argentina.Química Medicinal, Departamento de Ciencias Biológicas, UNLP, calle 47 y 115 (B1900BJW), La Plata, Argentina.
mmarder@qb.ffyb.uba.ar
A set of sulfamates and sulfamides designed, synthesized and evaluated against MES and PTZ tests with promising results
were tested for their affinity for the benzodiazepine binding site (BDZ-bs) in the GABAA receptor. The most active
compounds found; N,N´-dicyclohexylsulfamide (1) and N,N´-diphenethylsulfamide (2), competitively inhibited the binding
of [3H]-FNZ to the BDZ-bs with Ki ± SEM values of 27.7 ± 4.5 μM (n= 3) and 6.0 ± 1.2 μM (n= 3), respectively. The
behavioral actions of these sulfamides, i.p. administered in mice, were examined in the plus maze, hole board and locomotor
activity assays. Compound 1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters
measured in the hole board test (at 0.3, 1 and 3 mg/kg) and the plus maze assay (at 1 mg/kg). Compound 2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.A receptor. The most active
compounds found; N,N´-dicyclohexylsulfamide (1) and N,N´-diphenethylsulfamide (2), competitively inhibited the binding
of [3H]-FNZ to the BDZ-bs with Ki ± SEM values of 27.7 ± 4.5 μM (n= 3) and 6.0 ± 1.2 μM (n= 3), respectively. The
behavioral actions of these sulfamides, i.p. administered in mice, were examined in the plus maze, hole board and locomotor
activity assays. Compound 1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters
measured in the hole board test (at 0.3, 1 and 3 mg/kg) and the plus maze assay (at 1 mg/kg). Compound 2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.N,N´-dicyclohexylsulfamide (1) and N,N´-diphenethylsulfamide (2), competitively inhibited the binding
of [3H]-FNZ to the BDZ-bs with Ki ± SEM values of 27.7 ± 4.5 μM (n= 3) and 6.0 ± 1.2 μM (n= 3), respectively. The
behavioral actions of these sulfamides, i.p. administered in mice, were examined in the plus maze, hole board and locomotor
activity assays. Compound 1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters
measured in the hole board test (at 0.3, 1 and 3 mg/kg) and the plus maze assay (at 1 mg/kg). Compound 2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.3H]-FNZ to the BDZ-bs with Ki ± SEM values of 27.7 ± 4.5 μM (n= 3) and 6.0 ± 1.2 μM (n= 3), respectively. The
behavioral actions of these sulfamides, i.p. administered in mice, were examined in the plus maze, hole board and locomotor
activity assays. Compound 1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters
measured in the hole board test (at 0.3, 1 and 3 mg/kg) and the plus maze assay (at 1 mg/kg). Compound 2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters
measured in the hole board test (at 0.3, 1 and 3 mg/kg) and the plus maze assay (at 1 mg/kg). Compound 2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.2 evidenced
anxiolytic activity in the plus maze test at 1 mg/kg. Locomotor activity of mice was not modified by compound 1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.1 or 2 at the
doses tested. Anxiety represents a major problem for people with epilepsy. The use of these anticonvulsant sulfamides would
be beneficial to individuals who suffer from both disorders.