MUSCARINIC CHOLINERGIC RECEPTOR SUBTYPES IN HUMAN DETRUSOR MUSCLE STUDIED BY LABELED AND NONLABELED PIRENZEPINE, AFDX-116 AND 4DAMP

被引：26

作者：

KONDO, S

MORITA, T

TASHIMA, Y

机构：

[1] Second Department of Biochemistry, Akita University School of Medicine, Akita

[2] Department of Urology, Tokyo Medical and Dental University School of Medicine, Tokyo

来源：

UROLOGIA INTERNATIONALIS | 1995年 / 54卷 / 03期

关键词：

HUMAN DETRUSOR MUSCLE; MUSCARINIC RECEPTOR SUBTYPE; 3H-PIRENZEPINE; 3H-AFDX-116; 3H-4DAMP;

D O I：

10.1159/000282710

中图分类号：

R5 [内科学]; R69 [泌尿科学（泌尿生殖系疾病）];

学科分类号：

1002 ; 100201 ;

摘要：

The densities of M1, M2 and M3 muscarinic receptors in human detrusor muscle were measured using H-3-pirenzepine (H-3-PZP), H-3-AFDX-116 (H-3-AFDX) and H-3-4-diphenyl-acetoxy-N-methyl-piperidine methidide (H-3-4DAMP). The affinities of PZP, AFDX and 4DAMP for human detrusor were determined in inhibition experiments with H-3-quinuclidinyl benzilate (H-3-QNB). Saturation experiments with H-3-PZP, H-3-AFDX and H-3-4DAMP revealed the presence of M1, M2 and M3 receptors in human detrusor. The K-D values (nM) and the B-max values (fmol/mg protein) (mean +/- SD, n = 6) were 0.84 +/- 0.15 and 13.04 +/- 1.54 for H-3-PZP, 0.68 +/- 0.21 and 9.30 +/- 1.10 for H-3-AFDX, and 0.25 +/- 0.13 and 102.1 +/- 7.40 for H-3-4DAMP. These data indicate that the bladder muscarinic receptors consist mainly of the M3 subtype. Nonlabeled PZP, AFDX and 4DAMP inhibited the H-3-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.

引用

页码：150 / 153

页数：4

共 13 条

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