Garrett K M, Tabakoff B
Pharmacol Biochem Behav. 1985 Jun;22(6):985-92. doi: 10.1016/0091-3057(85)90307-7.
The postnatal development of benzodiazepine (BDZ) receptors was monitored in Heterogeneous Stock (HS) mice, and the BDZ receptors were characterized and categorized into Type I and Type II receptors. When the number of 3H-Flu binding sites (Bmax) was assessed at weekly intervals after the birth of the animal, the number of sites in both the cortex and cerebellum increased significantly if the data was expressed as fmol/mg tissue. On the other hand, no significant change in 3H-Flu binding sites was evidenced in the cortex, and the number of 3H-Flu binding sites in the cerebellum decreased during postnatal development if Bmax values were expressed as fmole/mg protein. When receptor binding data was analyzed for the presence of Type I and Type II BDZ receptors, the changes in KD values for 3H-Flu binding development could be accounted for by changes in relative proportions of Type I and Type II receptors present in the cortex and cerebellum during the maturation process. Type II receptors predominated in both cortex and cerebellum at birth, and Type I receptors proliferated primarily during the first two weeks of postnatal life. In the cortex of adult mice there were approximately equal numbers of Type I and Type II BDZ receptors. In the cerebellum of adult mice, computer assisted analysis of binding data could not distinguish the presence of two distinct BDZ binding sites. However, Hill coefficients and overall binding constants determined from data on CL-218,872 displacement of 3H-Flu binding to cerebellar membranes indicated that cerebellar tissue from adult mice did contain a heterogeneous array of BDZ receptors.
在异质种群(HS)小鼠中监测了苯二氮䓬(BDZ)受体的产后发育,并对BDZ受体进行了表征和分类为I型和II型受体。当在动物出生后每周评估3H-氟(3H-Flu)结合位点的数量(Bmax)时,如果数据以fmol/mg组织表示,皮质和小脑中的结合位点数量均显著增加。另一方面,如果Bmax值以fmole/mg蛋白质表示,皮质中3H-氟结合位点无显著变化,且在产后发育过程中小脑中3H-氟结合位点的数量减少。当分析受体结合数据以确定I型和II型BDZ受体的存在时,3H-氟结合发育的KD值变化可由成熟过程中皮质和小脑中I型和II型受体相对比例的变化来解释。出生时II型受体在皮质和小脑中均占主导,I型受体主要在出生后的前两周增殖。在成年小鼠的皮质中,I型和II型BDZ受体的数量大致相等。在成年小鼠的小脑中,对结合数据的计算机辅助分析无法区分两个不同的BDZ结合位点的存在。然而,根据CL-218,872对3H-氟与小脑膜结合的置换数据确定的希尔系数和总体结合常数表明,成年小鼠的小脑组织确实含有一系列异质性的BDZ受体。