Malminen O, Kontro P
Neurochem Res. 1986 Jan;11(1):85-94. doi: 10.1007/BF00965168.
The interactions of taurine and its precursor hypotaurine with the GABA-benzodiazepine receptor complex were studied by investigating their effects on GABA and flunitrazepam binding in rat brain membranes. Taurine, and to a lesser degree also hypotaurine, displaced the high- and low-affinity GABA binding. The maximal binding capacities of both sites were decreased in the presence of taurine, while the binding constants remained the same, suggesting noncompetitive interactions. Taurine and hypotaurine affected flunitrazepam binding only at a very high concentration (50 mmol/l), whereas GABA (within the concentration range of 0.1-100 mumol/l) significantly enhanced the binding. Taurine inhibited the GABA-stimulated binding dose-dependently. These modulatory effects of taurine on the GABA-benzodiazepine receptor complex could result from interactions with the GABA recognition site but not from direct actions on the benzodiazepine site.
通过研究牛磺酸及其前体次牛磺酸对大鼠脑膜中γ-氨基丁酸（GABA）和氟硝西泮结合的影响，对它们与GABA-苯二氮䓬受体复合物的相互作用进行了研究。牛磺酸以及程度较轻的次牛磺酸，取代了高亲和力和低亲和力的GABA结合。在牛磺酸存在的情况下，两个位点的最大结合容量均降低，而结合常数保持不变，提示存在非竞争性相互作用。牛磺酸和次牛磺酸仅在非常高的浓度（50 mmol/L）时影响氟硝西泮结合，而GABA（在0.1 - 100 μmol/L浓度范围内）显著增强结合。牛磺酸剂量依赖性地抑制GABA刺激的结合。牛磺酸对GABA-苯二氮䓬受体复合物的这些调节作用可能源于与GABA识别位点的相互作用，而非对苯二氮䓬位点的直接作用。
