苯二氮卓类药物与γ-氨基丁酸（GABA）受体在功能上相关：体内的进一步电生理证据。

Benzodiazepine and gaba receptors are functionally related: further electrophysiological evidence in vivo.

Nestoros J N

Prog Neuropsychopharmacol Biol Psychiatry. 1982;6(4-6):417-20. doi: 10.1016/s0278-5846(82)80119-x.

Abstract

The effects of five benzodiazepines (Ro 21-3981, flurazepam, chlordiazepoxide, medazepam and clozapine) on GABA-mediated electrically-evoked cortical inhibition were tested. 2. These five drugs were chosen because their solubility in water allows their microiontophoresis and because their relative affinities for the benzodiazepine receptor in rat brain membranes have been measured. 3. When tested with equal iontophoretic doses in 11 different neurons, the degree of potentiation of electrically evoked cortical inhibition produced by these benzodiazepines correlated significantly (r = -0.60704; p less than 0.01; phi = 33) with the logarithm of the Ki values of these drugs for inhibiting specific 3H-diazepam binding to rat brain membranes. 4. When tested with iontophoretic doses which were directly proportional to their Ki values for inhibiting 3H-diazepam binding to rat brain membranes, these benzodiazepines produced very similar potentiations of electrically evoked cortical inhibition.

摘要

测试了五种苯二氮䓬类药物（Ro 21-3981、氟西泮、氯氮卓、美达西泮和氯氮平）对γ-氨基丁酸（GABA）介导的电诱发皮质抑制的影响。2. 选择这五种药物是因为它们在水中的溶解度允许进行微量离子电泳，并且已经测量了它们对大鼠脑膜中苯二氮䓬受体的相对亲和力。3. 当在11个不同的神经元中以相等的离子电泳剂量进行测试时，这些苯二氮䓬类药物产生的电诱发皮质抑制的增强程度与这些药物抑制[3H]地西泮与大鼠脑膜特异性结合的Ki值的对数显著相关（r = -0.60704；p < 0.01；φ = 33）。4. 当以与它们抑制[3H]地西泮与大鼠脑膜结合的Ki值成正比的离子电泳剂量进行测试时，这些苯二氮䓬类药物产生了非常相似的电诱发皮质抑制增强作用。