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目的验证受体结合试验检测的糖皮质激素受体(GR)的特异性,从受体水平探索皮质类固醇性青光眼治疗的新途径。方法用Ru38486,通过受体的竞争抑制试验,检测皮质类固醇性青光眼患者、正常人外周血淋巴细胞GR的半数抑制量(IC50)和平衡抑制常数(KI),并将检测结果作统计分析。结果皮质类固醇性青光眼患者、正常人外周血淋巴细胞GR的IC50分别为(224.30±18.79)nmol/L和(195.99±16.08)nmol/L,KI分别为(44.56±5.10)nmol/L和(37. 88±2.79)nmol/L,差异均有显著性( P <0.05);两组样本的竞争抑制曲线为“S”形。结论受体结合试验检测的GR为糖皮质激素(GC)特异性受体,从受体的竞争性角度证明皮质类固醇性青光眼患者外周血淋巴细胞GR的结合位点高于正常人,GR特性检测可能成为皮质类固醇性青光眼诊断和鉴别诊断的客观标准,GR拮抗剂可望发展成为治疗皮质类固醇性青光眼和其他类型青光眼的新途径。
Objective To verify the specificity of glucocorticoid receptor (GR) detected by receptor binding assay and to explore new ways of treating corticosteroid glaucoma at receptor level. Methods The inhibitory activity (IC50) and equilibrium inhibition constant (KI) of GR in peripheral blood lymphocytes of corticosteroid-induced glaucoma patients and normal persons were detected by Ru38486, a competitive inhibition test of the receptor, and the results were statistically analyzed. Results The IC50 of peripheral blood lymphocytes in normal controls were (224.30 ± 18.79) nmol / L and (195.99 ± 16.08) nmol / L, respectively, and KI were (44.56 ± 5.10) nmol / L and 88 ± 2.79) nmol / L, the difference was significant (P <0.05). The competitive inhibition curve of the two groups was “S”. Conclusions The receptor binding assay (GR) is a specific receptor for glucocorticoid (GC). From the competitive perspective of the receptor, GR binding sites in peripheral blood lymphocytes in patients with corticosteroid glaucoma were higher than those in normal subjects. May become an objective standard for the diagnosis and differential diagnosis of corticosteroid-induced glaucoma. GR antagonists are expected to develop into new avenues for the treatment of corticosteroid glaucoma and other types of glaucoma.