Kondo S, Morita T, Hirano S
Second Department of Biochemistry, Akita University School of Medicine.
J Smooth Muscle Res. 1993 Apr;29(2):63-8. doi: 10.1540/jsmr.29.63.
The affinities of various muscarinic antagonists to human detrusor muscle were determined using radioligand binding techniques. Saturation experiments with 3H-QNB revealed that there were significant amount of muscarinic cholinergic receptors in human detrusor muscle. Displacement of 3H-QNB binding by various muscarinic subtype selective drugs was studied in the inhibition experiment. Pirenzepine, AFDX-116 and 4-DAMP inhibited the 3H-QNB binding to human detrusor muscle with the Ki values (nM) (mean +/- S.D., n = 6) of 243 +/- 62.5, 59.7 +/- 15.3 and 2.69 +/- 0.96, respectively. These data indicate that M3-selective drug possesses the highest affinity to human detrusor muscle. The Ki values of oxybutynin and tiquizium bromide were similar to those of 4-DAMP, suggesting that these two drugs have strong affinities to human detrusor muscle.
利用放射性配体结合技术测定了各种毒蕈碱拮抗剂与人逼尿肌的亲和力。用³H-QNB进行的饱和实验表明，人逼尿肌中存在大量毒蕈碱胆碱能受体。在抑制实验中研究了各种毒蕈碱亚型选择性药物对³H-QNB结合的置换作用。哌仑西平、AFDX-116和4-DAMP抑制³H-QNB与人逼尿肌的结合，其Ki值（纳摩尔）（平均值±标准差，n = 6）分别为243±62.5、59.7±15.3和2.69±0.96。这些数据表明，M3选择性药物与人逼尿肌的亲和力最高。奥昔布宁和曲司氯铵的Ki值与4-DAMP相似，表明这两种药物与人逼尿肌有很强的亲和力。
