Goetz C, Bourgoin S, Cesselin F, Brandi A, Bression D, Martinet M, Peillon F, Hamon M
INSERM U 114, Collège de France, 11, Place M. Berthelot, 75231 Paris Cedex 05, France.
Neurochem Int. 1983;5(4):375-83. doi: 10.1016/0197-0186(83)90066-9.
The subcutaneous implantation of an estradiol pellet (10 mg) into female rats induced a hypophyseal hyperplasia with hyperprolactinaemia. Examination of neurotransmitter receptors in the hippocampus, striatum and cerebral cortex one month after the implantation revealed that estrogenization was associated with: an increased density of (3)H-domperidone binding sites (D(2) receptors) in the striatum and reduced numbers of (3)H-serotonin high affinity sites (5-HT(1) receptors) in the hippocampus and of (3)H-muscimol binding sites (GABA receptors) in the hippocampus, striatum and cerebral cortex. In contrast, the characteristics of (3)H-spiperone binding to 5-HT(2) receptors (in the cerebral cortex) and those of (3)H-flunitrazepam binding to benzodiazepine sites (in the three brain regions examined) were not significantly different in estrogenized and in control female rats. However, the enhancing effect of GABA on (3)H-flunitrazepam binding was markedly reduced in brain membranes from estrogenized animals. The respective roles of estradiol and prolactin in mediating these changes in neurotransmitter receptors are discussed notably with regard to the regional heterogeneity of estradiol binding capacity in the rat brain.
将雌二醇药丸（10毫克）皮下植入雌性大鼠体内会诱发垂体增生并伴有高催乳素血症。植入后一个月对海马体、纹状体和大脑皮层中的神经递质受体进行检查发现，雌激素化与以下情况相关：纹状体中（3）H-多潘立酮结合位点（D（2）受体）密度增加，海马体中（3）H-5-羟色胺高亲和力位点（5-HT（1）受体）数量减少，海马体、纹状体和大脑皮层中（3）H-蝇蕈醇结合位点（GABA受体）数量减少。相比之下，雌激素化雌性大鼠和对照雌性大鼠大脑皮层中（3）H-螺哌隆与5-HT（2）受体的结合特性以及三个脑区中（3）H-氟硝西泮与苯二氮䓬位点的结合特性并无显著差异。然而，雌激素化动物脑膜中GABA对（3）H-氟硝西泮结合的增强作用明显降低。文中特别讨论了雌二醇和催乳素在介导神经递质受体这些变化中的各自作用，尤其是关于大鼠脑中雌二醇结合能力的区域异质性。
