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目的 研究人逼尿肌细胞中肾上腺素能 β3 受体的表达及功能。 方法 采用细胞功能试验、放射性配基结合及RT PCR方法检测肾上腺素能 β受体在人逼尿肌细胞中的表达情况及对逼尿肌收缩的影响。 结果 逼尿肌中可检测到 3种 β受体亚型的mRNA ;非选择性 β受体激动剂产生的最大松弛效能为腺苷酸环化酶激活剂 (forsklin ,10 -5mol/L)的 (77.2± 2 .5 ) % ,pD2值为6 .0 2± 0 .2 2。β1、β2 受体激动剂对逼尿肌松弛作用无显著影响 ;β3 受体激动剂BRL37344和CGP12 177A产生的松弛作用分别为forsklin的 (48.2± 2 .1) %和 (47.8± 5 .3) % ,pD2 值分别为 6 .32± 0 .15和4 7.8± 5 .3,内在活性 (IA)分别为 0 .5 4± 0 .0 5和 0 .4 9± 0 .0 4。 结论 人逼尿肌细胞中存在 3种受体亚型的mRNA ,β3 亚型对介导逼尿肌松弛起主要作用
Objective To study the expression and function of adrenergic β3 receptor in human detrusor. Methods The expression of adrenergic receptor β in human detrusor myocytes and the effect on detrusor contraction were detected by cell function test, radioligand binding and RT PCR. Results The mRNA of three β receptor subtypes was detected in the detrusor muscle. The maximum relaxation efficiency of non-selective β-agonist was deoxyuridine (10 -5 mol / L) (77.2 ± 2.5%), pD2 value was 6.022 ± 0.22. β1 and β2 receptor agonists had no significant effect on detrusor relaxation; the relaxation effects of β3 receptor agonists BRL37344 and CGP12177A were (48.2 ± 2.1)% and (47.8 ± 5.3) forsklin, respectively %, pD2 values were 6 .32 ± 0 .15 and 4 7.8 ± 5 .3 respectively, and the intrinsic activity (IA) was respectively 0 .54 ± 0. 05 and 0 .49 ± 0 .0 4. Conclusion Human detrusor myocytes have mRNAs of three receptor subtypes, and β3 subtype plays a major role in mediating detrusor relaxation