6-甲基-3'-溴黄酮，一种对GABA(A)受体苯二氮䓬结合位点具有高亲和力且具有一定拮抗特性的配体。

6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.

作者信息

Viola H, Marder M, Nuñez J, Izquierdo L, Wasowski C, Wolfman C, Ardenghi P, Barros D, Medina J H, Paladini A C

机构信息

Facultad de Medicina, Instituto de Biología Celular, Paraguay 2155 (1121), Buenos Aires, Argentina.

出版信息

Biochem Biophys Res Commun. 1999 Sep 7;262(3):643-6. doi: 10.1006/bbrc.1999.1273.

DOI:10.1006/bbrc.1999.1273

PMID:10471378

Abstract

6-Methyl-3'-bromoflavone inhibited [(3)H]flunitrazepam binding to the benzodiazepine binding site of the GABA(A) receptor (BDZ-bs) with Ki values between 10 and 50 nM in different brain regions. The GABA ratio of 1.03 for [(3)H]flunitrazepam binding to cerebral cortex, 0.76 for cerebellum, 0.7 for hippocampus, 0.7 for striatum, and 0.8 for spinal cord indicated an antagonistic or weak inverse agonistic profile of 6-methyl-3'-bromoflavone on BDZ-bs. Unlike classical benzodiazepines, it had no anticonvulsant, anxiolytic, myorelaxant, sedative, amnestic or motor incoordination effects. However, it antagonized the muscle relaxant, the sedative effect, and the changes in locomotor activity induced by diazepam. Taken together, these findings suggest that 6-methyl-3'-bromoflavone has an antagonistic profile on the BDZ-bs.

摘要

6-甲基-3'-溴黄酮抑制[(3)H]氟硝西泮与GABA(A)受体的苯二氮䓬结合位点（BDZ-bs）结合，在不同脑区的Ki值介于10至50 nM之间。[(3)H]氟硝西泮与大脑皮层结合的GABA比率为1.03，小脑为0.76，海马体为0.7，纹状体为0.7，脊髓为0.8，表明6-甲基-3'-溴黄酮对BDZ-bs具有拮抗或弱反向激动作用。与经典苯二氮䓬不同，它没有抗惊厥、抗焦虑、肌松、镇静、遗忘或运动不协调作用。然而，它拮抗了地西泮诱导的肌肉松弛、镇静作用以及运动活动的变化。综上所述，这些发现表明6-甲基-3'-溴黄酮对BDZ-bs具有拮抗作用。