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以~3H地塞米松(Dex)为特异性配基,以一点分析法测得大白鼠腹腔中性粒细胞(PMNs)的糖皮质激素受体(GCR)位点数为5270±216/个PMN(n=18,X±SE下同);体外实验,PMNs直接与山莨菪碱(654-23×10~(-5)M)温育,对GCR无明显影响,测得位点数为4896±360/个PMNs(n=20,P>0.4);体内实验表明,给大鼠肌肉注射654-2(10mg/kg)每日两次共二天,则GCR位点数降至2740±101/个PMNs(n=18,P<0.001)。此时还测得血浆皮质酮含量明显增高(P<0.01)。提示654-2对GCR的影响可能与增加皮质激素所致的“降调节”有关。
Using 3H-dexamethasone (Dex) as the specific ligand, the number of glucocorticoid receptor (GCR) sites in rat peritoneal neutrophils (PMNs) measured by one-point analysis was 5270 ± 216 / PMN n = 18 and X ± SE). In vitro experiments, PMNs incubated directly with anisodamine (654-23 × 10 -5 M) had no significant effect on GCR, and the number of loci was 4896 ± 360 / PMNs (n = 20, P> 0.4). In vivo experiments showed that intramuscular injection of 654-2 (10 mg / kg) twice a day in rats for two days reduced the number of GCR sites to 2740 ± 101 per PMNs n = 18, P <0.001). The plasma corticosterone level was also significantly increased at this time (P <0.01). Tip 654-2 on the GCR may be related to increased corticosteroid-induced “down regulation.”