Abstract：
:A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-diphenethylsulfamide (10), competitively inhibited the binding of [(3)H]-flunitrazepam to the benzodiazepine binding site with K(i)±SEM values of 27.7±4.5μM (n=3) and 6.0±1.2μM (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 7 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters measured in the hole-board test (at 1 and 3mg/kg) and the plus-maze assay (at 1 and 3mg/kg). Compound 10 evidenced anxiolytic activity in the plus-maze and the hole-board tests at 1mg/kg. Locomotor activity of mice was not modified by compound 7 or 10 at the doses tested. Flumazenil, a non selective benzodiazepine binding site antagonist, was able to completely reverse the anxiolytic-like effects of these sulfamides, proving that the GABA(A) receptor is implicated in this action. Anxiety represents a major problem for people with epilepsy. The use of anxiolytic and anticonvulsant sulfamides would be beneficial to individuals who suffer from both disorders.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Wasowski C,Gavernet L,Barrios IA,Villalba ML,Pastore V,Samaja G,Enrique A,Bruno-Blanch LE,Marder Mdoi
10.1016/j.bcp.2011.10.015subject
Has Abstractpub_date
2012-01-15 00:00:00pages
253-9issue
2eissn
0006-2952issn
1873-2968pii
S0006-2952(11)00789-1journal_volume
83pub_type
杂志文章abstract：:Diclofenac is a non-steroidal anti-inflammatory drug that is widely used clinically but side effects associated with the administration of the drug have been reported. The apoptotic effect of the drug has been evaluated in human and rat hepatocytes. Apoptosis was observed after exposure to sub-cytotoxic concentrations...
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pub_type： 杂志文章
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更新日期：2008-10-01 00:00:00
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pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
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更新日期：1982-08-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(83)90196-x
更新日期：1983-11-01 00:00:00
