Petrillo P, La Regina A, Sbacchi M, Tavani A, Robson L E, Kosterlitz H W
Istituto di Ricerche Farmacologiche Mario Negri, Milano, Italy.
Eur J Pharmacol. 1989 Jul 18;166(2):213-7. doi: 10.1016/0014-2999(89)90061-7.
The highest maximum binding capacities at the mu-sites of rabbit brain are in the striatum, with intermediate levels in the diencephalon, mesencephalon, cerebellum and cortex and low levels in the pons-medulla and hippocampus. For the delta-site the highest maximum binding capacity is also in the striatum; there are almost equally low levels in the other brain regions. At the kappa-sites the maximum binding capacities are highest in the diencephalon; there are intermediate levels in the cortex and striatum, and low levels in the mesencephalon, cerebellum, hippocampus and pons-medulla. The KD values lack reproducibility; there are no regional variations at the kappa-site as estimated with 3H-bremazocine, but the possibility cannot be excluded that there are regional variations in the KD values for [3H][D-Ala2,MePhe4,Gly-ol5]enkephalin at the mu-site or for [3H][D-Ala2,D-Leu5]enkephalin at the delta-site. It may be important to use saturation analysis in future investigations of the distributions of the binding sites.
兔脑μ位点的最大结合能力最高的部位是纹状体,间脑、中脑、小脑和皮质的结合能力处于中等水平,脑桥-延髓和海马的结合能力较低。对于δ位点,最大结合能力最高的部位同样是纹状体;其他脑区的结合能力几乎同样低。对于κ位点,最大结合能力在间脑最高;皮质和纹状体的结合能力处于中等水平,中脑、小脑、海马和脑桥-延髓的结合能力较低。解离常数(KD)值缺乏可重复性;用3H-布马佐辛评估时,κ位点没有区域差异,但不能排除在μ位点[3H][D-丙氨酸2,甲基苯丙氨酸4,甘醇5]脑啡肽或在δ位点[3H][D-丙氨酸2,D-亮氨酸5]脑啡肽的KD值存在区域差异的可能性。在未来对结合位点分布的研究中使用饱和分析可能很重要。