Fomenko A I, Parkhomets P K, Stepanenko S P, Donchenko G V
Ukr Biokhim Zh (1978). 1994 Jul-Aug;66(4):75-80.
Bicucculine being introduced to rats has induced an increase of [14C]GABA capture with synaptosomes and simultaneous decrease of GABA and NAD level in the brain. The decrease of the inhibiting effect of GABA is accompanied by the increase of specific binding of [3H]flunitrazepam with benzodiazepine receptors at the expense of the increase of binding capacity from 0.33 to 0.45 g/mol per 100 mg of protein. Under these conditions the dissociation constant remains unchanged. Such an activation of benzodiazepine receptors was observed under the lack of NAD in the organism (model of PP-hypovitaminosis). Introduction of the surplus doses of nicotinamide neutralizes the convulsant effect on benzodiazepine receptors.
将荷包牡丹碱引入大鼠体内已导致脑内突触体对[14C]GABA摄取增加,同时脑内GABA和NAD水平降低。GABA抑制作用的降低伴随着[3H]氟硝西泮与苯二氮䓬受体特异性结合的增加,代价是结合能力从每100毫克蛋白质0.33克/摩尔增加到0.45克/摩尔。在这些条件下,解离常数保持不变。在机体缺乏NAD的情况下(糙皮病-维生素缺乏症模型)观察到了苯二氮䓬受体的这种激活。引入过量剂量的烟酰胺可中和对苯二氮䓬受体的惊厥作用。