Effects of Valeriana officinalis extracts on [3H]flunitrazepam binding, synaptosomal [3H]GABA uptake, and hippocampal [3H]GABA release
Effects of Valeriana officinalis extracts on [3H]flunitrazepam binding, synaptosomal [3H]GABA uptake, and hippocampal [3H]GABA release
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DOI：
10.1023/a:1022576405534
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发表时间：
1999-11-01
影响因子：
4.4
通讯作者：
Chavez, P
中科院分区：
文献类型：
--
作者：
Ortiz, JG;Nieves-Natal, J;Chavez, P
缬草提取物因其镇静、催眠、安定和抗惊厥作用而被用于民间医药，并可能与γ-氨基丁酸（GABA）和/或苯二氮卓类位点相互作用。在低浓度下，缬草提取物增强[H-3]氟硝西泮结合（EC 50 4.13 x 10（-10）mg/ml）。然而，这种增加的[H-3]氟硝西泮结合被更高浓度下的抑制所取代（IC 50为4.82 x 10（-1）mg/ml）。这些结果与存在与[H-3]氟硝西泮结合位点相互作用的至少两种不同生物活性一致。缬草提取物也增强K+或藜芦碱刺激的[H-3]GABA预载海马切片的放射性释放。最后，抑制突触体[H-3]GABA摄取的缬草提取物也显示了与古瓦辛的双相相互作用。结果证实，缬草提取物对GABAA受体有影响，但也可以在GABA能神经元的其他突触前成分相互作用。
Extracts of Valeriana officinalis have been used in folkloric medicine for its sedative, hypnotic, tranquilizer and anticonvulsant effects, and may interact with gamma-aminobutyric acid (GABA) and/or benzodiazepine sites. At low concentrations, valerian extracts enhance [H-3]flunitrazepam binding (EC50 4.13 x 10(-10) mg/ml). However, this increased [H-3]flunitrazepam binding is replaced by an inhibition at higher concentrations (IC50 Of 4.82 x 10(-1) mg/ml). These results are consistent with the presence of at least two different biological activities interacting with [H-3]flunitrazepam binding sites. Valerian extracts also potentiate K+ or veratridine-stimulated release of radioactivity from hippocampal slices preloaded with [H-3]GABA. Finally, inhibition of synaptosomal [H-3]GABA uptake by valerian extracts also displays a biphasic interaction with guvacine. The results confirm that valerian extracts have effects on GABAA receptors, but can also interact at other presynaptic components of GABAergic neurons.