Fomenko A I, Parkhomets P K, Stepanenko S P, Donchenko G V
Ukr Biokhim Zh (1978). 1991 May-Jun;63(3):65-9.
The receptor protein solubilized from synaptic membranes specifically binds [14C] NAD (dissociation constant--0.75 microM, capacity of binding sites--0.0125 nmol of metaid per 1 mg of protein). All the studied benzodiazepines (phenazepam, nitrazepam, clonazepam, flunitrazepam) are able to displace [14C] NAD from its receptor sites, the mixed type of inhibition being manifested. An inhibition constant for flunitrazepam, a ligand of benzodiazepine receptors, equals 10 microM. GABA promotes an inhibiting effect of benzodiazepines. It is supposed that neurotropic action of NAD is realized through the GABA-benzodiazepine complex of neuronal membranes.
从突触膜中溶解出来的受体蛋白能特异性结合[14C]NAD（解离常数——0.75微摩尔，结合位点容量——每1毫克蛋白质0.0125纳摩尔甲碘）。所有研究的苯二氮䓬类药物（非那西泮、硝西泮、氯硝西泮、氟硝西泮）都能从其受体位点取代[14C]NAD，表现出混合型抑制作用。苯二氮䓬受体配体氟硝西泮的抑制常数为10微摩尔。γ-氨基丁酸（GABA）能增强苯二氮䓬类药物的抑制作用。据推测，NAD的神经otropic作用是通过神经元膜的GABA-苯二氮䓬复合物实现的。
