Kondo S, Morita T, Tashima Y
Second Department of Biochemistry, Akita University School of Medicine, Japan.
Urol Int. 1995;54(3):150-3. doi: 10.1159/000282710.
The densities of M1, M2 and M3 muscarinic receptors in human detrusor muscle were measured using 3H-pirenzepine (3H-PZP), 3H-AFDX-116 (3H-AFDX) and 3H-4-diphenyl-acetoxy-N-methyl-piperidine methidide (3H-4DAMP). The affinities of PZP, AFDX and 4DAMP for human detrusor were determined in inhibition experiments with 3H-quinuclidinyl benzilate (3H-QNB). Saturation experiments with 3H-PZP, 3H-AFDX and 3H-4DAMP revealed the presence of M1, M2 and M3 receptors in human detrusor. The KD values (nM) and the Bmax values (fmol/mg protein) (mean +/- SD, n = 6) were 0.84 +/- 0.15 and 13.04 +/- 1.54 for 3H-PZP, 0.68 +/- 0.21 and 9.30 +/- 1.10 for 3H-AFDX, and 0.25 +/- 0.13 and 102.1 +/- 7.40 for 3H-4DAMP. These data indicate that the bladder muscarinic receptors consist mainly of the M3 subtype. Nonlabeled PZP, AFDX and 4DAMP inhibited the 3H-QNB binding to human detrusor with Ki values (nM) (mean +/- SD, n = 6) of 243 +/- 62.5, 59.7 +/- 15.3, 2.69 +/- 0.96, respectively. Human detrusor was found to have a high affinity for 4DAMP. These data suggest that M3 muscarinic receptors are biochemically predominant in human detrusor muscle.
使用3H-哌仑西平（3H-PZP）、3H-AFDX-116（3H-AFDX）和3H-4-二苯基乙酰氧基-N-甲基哌啶甲基碘（3H-4DAMP）测量人逼尿肌中M1、M2和M3毒蕈碱受体的密度。在3H-喹核醇基苯甲酸酯（3H-QNB）抑制实验中测定了PZP、AFDX和4DAMP对人逼尿肌的亲和力。用3H-PZP、3H-AFDX和3H-4DAMP进行的饱和实验揭示了人逼尿肌中存在M1、M2和M3受体。3H-PZP的KD值（nM）和Bmax值（fmol/mg蛋白）（平均值±标准差，n = 6）分别为0.84±0.15和13.04±1.54,3H-AFDX为0.68±0.21和9.30±1.10，3H-4DAMP为0.25±0.13和102.1±7.40。这些数据表明膀胱毒蕈碱受体主要由M3亚型组成。未标记的PZP、AFDX和4DAMP抑制3H-QNB与人逼尿肌的结合，Ki值（nM）（平均值±标准差，n = 6）分别为243±62.5、59.7±15.3、2.69±0.96。发现人逼尿肌对4DAMP具有高亲和力。这些数据表明M3毒蕈碱受体在人逼尿肌中在生化上占主导地位。
