Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists

被引：16
作者：
Grasso, S
Micale, N
Zappalá, M
Galli, A
Costagli, C
Menniti, FS
De Micheli, C
机构：
[1] Univ Milan, Ist Chim Farmaceut, I-20131 Milan, Italy
[2] Pfizer Global Res & Dev, Groton, CT 06340 USA
[3] Univ Florence, Dipartimento Farmacol Preclin & Clin, I-50134 Florence, Italy
[4] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 03期
关键词：
D O I：
10.1016/S0960-894X(02)00955-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A selected set of I -aryl-7,8-methylenedioxy-2,3-benzodiazepin-4-ones and their analogues were evaluated for their ability to bind the competitive and noncompetitive sites of the AMPA receptors complex as well as to the glycine site of the NMDA receptors. The results put in evidence that most of the test compounds, despite a close structural similarity with GYKI 52466, possess a significantly different pharmacological profile. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：443 / 446
页数：4
相关论文
共 21 条
[1]  
[Anonymous], DRUG NEWS PERSPECT
[2]   AMPA receptor agonists, antagonists and modulators: their potential for clinical utility [J].
Bigge, CF ;
Nikam, SS .
EXPERT OPINION ON THERAPEUTIC PATENTS, 1997, 7 (10) :1099-1114
[3]   Ligands for glutamate receptors:: Design and therapeutic prospects [J].
Bräuner-Osborne, H ;
Egebjerg, J ;
Nielsen, EO ;
Madsen, U ;
Krogsgaard-Larsen, P .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) :2609-2645
[4]   Synthesis and biological evaluation of a series of quinazoline-2-carboxylic acids and quinazoline-2,4-diones as glycine-NMDA antagonists: A pharmacophore model based approach [J].
Colotta, V ;
Catarzi, D ;
Varano, F ;
Cecchi, L ;
Filacchioni, G ;
Galli, A ;
Costagli, C .
ARCHIV DER PHARMAZIE, 1997, 330 (05) :129-134
[5]   7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists [J].
De Sarro, A ;
De Sarro, G ;
Gitto, R ;
Grasso, S ;
Micale, N ;
Quartarone, S ;
Zappala, M .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (08) :971-976
[6]   Synthesis and anticonvulsant activity of new 2,3-benzodiazepines as AMPA receptor antagonists [J].
De Sarro, A ;
De Sarro, G ;
Gitto, R ;
Grasso, S ;
Micale, N ;
Zappalà, M .
FARMACO, 1999, 54 (03) :178-187
[7]  
Dingledine R, 1999, PHARMACOL REV, V51, P7
[8]  
Gill R, 1997, INT REV NEUROBIOL, V40, P197
[9]  
Gorter JA, 1997, J NEUROSCI, V17, P6179
[10]   Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones [J].
Grasso, S ;
De Sarro, G ;
De Sarro, A ;
Micale, N ;
Polimeni, S ;
Zappalà, M ;
Puia, G ;
Baraldi, M ;
De Micheli, C .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (04) :463-466
123