Ethanol enhances [3H]diazepam binding at the benzodiazepine-GABA-receptor-ionophore complex.
Ethanol enhances [3H]diazepam binding at the benzodiazepine-GABA-receptor-ionophore complex.
复制标题
乙醇增强[3H]地西泮与苯二氮卓-GABA-受体-离子载体复合物的结合。
DOI：
10.1016/0014-2999(80)90519-1
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发表时间：
1980
影响因子：
5
通讯作者：
Ticku,MK
中科院分区：
文献类型：
--
作者：
Burch,TP;Ticku,MK
乙醇的药理学特征与苯二氮卓类和巴比妥类药物非常相似。因此，乙醇具有抗焦虑、镇静催眠和肌肉松弛的作用。乙醇（Nestoros，1980），像苯二氮卓类和巴比妥类药物，已被证明与~-氨基丁酸（GABA）介导的突触抑制性传递相互作用。我们的研究还表明，GABA受体敏感性在急性和慢性乙醇治疗后以及在其戒断期间发生改变（Ticku，1980）。最近，巴比妥类药物已显示出（a）增强苯二氮卓结合（Leeb-Lundberg et al.，1980）和（B）增强GABA诱导的地西泮结合的增加（Skolnick等，1980年）。在这份报告中，我们研究了乙醇与[~ H]地西泮结合的相互作用。用Brinkman Polytron将脑组织置于50体积的含有0.2M NaCl，5 mM磷酸钠，pH 7的冰冷缓冲液中，在设定值为5的条件下，通过两次15秒的爆发，从成年雄性Sprague-Dawley大鼠制备大鼠脑膜（减去脑桥髓质）。然后将匀浆以750× g离心10 min。
Ethanol has a pharmacological profile very similar to that of benzodiazepines and barbiturates. Thus, ethanol has antianxiety, sedative-hypnotic and muscle relaxant effects. Ethanol (Nestoros, 1980), like benzodiazepines and barbiturates, has been shown to interact with the synaptic inhibitory transmission mediation by~-aminobutyric acid (GABA). Our studies have also shown that GABA receptor sensitivity is altered following acute and chronic ethanol treatments and during its withdrawal (Ticku, 1980).Recently, barbiturates have been shown to (a) enhance benzodiazepine binding (Leeb-Lundberg et al., 1980) and (b) potentiate GABA-induced increases in diazepam binding (Skolnick et al., 1980). In this report, we have investigated the interaction of ethanol with [~ H] diazepam binding. Rat brain membranes (minus ponsmedulla) were prepared from adult male Sprague-Dawley rats by homogenizing the brain tissue in 50 vol of ice cold buffer containing 0.2 M NaC1, 5 mM sodium phosphate, pH 7, with a Brinkman Polytron, by two 15 sec bursts at a setting of 5. The homogenate was then centrifuged at 750× g for 10 min. The supernatant was then cen-