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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Pharmacological characterization of 6-bromo-3'-nitroflavone, a synthetic flavonoid with high affinity for the benzodiazepine receptors.
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Pharmacological characterization of 6-bromo-3'-nitroflavone, a synthetic flavonoid with high affinity for the benzodiazepine receptors.

机译：6-溴-3'-硝基黄酮（对苯二氮杂receptor受体具有高亲和力的合成类黄酮）的药理特性。

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摘要

6-Bromo-3'-nitroflavone is a synthetic flavone derivative that selectively recognizes benzodiazepine receptors and has potent anxiolytic-like effects. Here, we describe in detail its pharmacological characterization. When i.p. injected in mice, 6-bromo-3'-nitroflavone (0.01-0.3 mg/kg) had an anxiolytic-like effect in the elevated plus-maze test. This effect was blocked by the specific benzodiazepine receptor antagonist, flumazenil. In addition, it exhibited anxiolytic-like actions when given orally (1 mg/kg). 6-Bromo-3'-nitroflavone did not exhibit myorelaxant effects (up to 30 mg/kg, i.p.). Unlike diazepam, this flavonoid produced no anterograde amnesia in a one-trial inhibitory avoidance learning. On the other hand, 6-bromo-3'-nitroflavone possessed mild anticonvulsant activity (0.1 mg/kg, i.p.) and provoked sedative-depressant actions only at doses 100-1000 times higher than those producing anxiolytic-like effects. 6-Bromo-3'-nitroflavone (0.1-1 mM) produced a lower potentiation of gamma-amino-butyric acid (GABA)-stimulated 36Cl- influx (126-138%) in comparison to diazepam (0.1 mM: 166%) in cerebral cortical membrane vesicles. Taken together, these findings suggest that 6-bromo-3'-nitroflavone has anxiolytic-like action possibly behaving as a partial agonist of the benzodiazepine receptors.
机译：6-溴-3'-硝基黄酮是一种合成的黄酮衍生物，可选择性识别苯并二氮杂ze受体，并具有类似抗焦虑的作用。在这里，我们详细描述其药理特性。当i.p.在小鼠体内注射6-溴3'-硝基黄酮（0.01-0.3 mg / kg）在高迷宫试验中具有抗焦虑样作用。特定的苯二氮卓受体拮抗剂氟马西尼阻断了该作用。此外，口服（1 mg / kg）时，它表现出类似抗焦虑的作用。 6-Bromo-3'-硝基黄酮没有表现出肌肉松弛作用（最高30 mg / kg，腹膜内）。与地西epa不同，这种黄酮在一次抑制性回避学习中不会产生顺行性健忘症。另一方面，6-溴-3'-硝基黄酮具有温和的抗惊厥活性（0.1 mg / kg，腹腔注射），并且其镇静镇静作用仅比产生抗焦虑作用的剂量高100-1000倍。与地西epa（0.1 mM：166％）相比，6-Bromo-3'-硝基黄酮（0.1-1 mM）产生了较低的γ-氨基丁酸（GABA）刺激的36Cl-内流（126-138％）。在大脑皮层膜囊泡中。综上所述，这些发现表明6-溴-3'-硝基黄酮具有象苯二氮卓受体的部分激动剂一样的抗焦虑作用。

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