6β-乙酰氧基去甲托烷对人和豚鼠气道的收缩作用。

Contractile effect of 6 beta-acetoxy nortropane on human and guinea pig airways.

作者信息

Zhang Y, Moreau J, Molimard M, Naline E, Bisson A, Advenier C

机构信息

Faculté de Médecine Paris-Ouest, France.

出版信息

Zhongguo Yao Li Xue Bao. 1998 May;19(3):211-7.

PMID:10375728

Abstract

AIM

To study the effects of 6 beta-acetoxy nortropane (6 beta-AN) on the isolated human bronchus and guinea pig trachea.

METHODS

The contractile effect of 6 beta-AN was studied with 4 different muscarinic receptor antagonists on airway strips and inositol phosphates (IP) accumulation in human bronchi was determined by HPLC with radioactivity flow detector.

RESULTS

(1) The maximal contractile effect of 6 beta-AN was lower than that of acetylcholine (ACh) on the human bronchus and equal to that of ACh on the guinea pig trachea. 6 beta-AN was more potent than ACh on both preparations (68 and 245 times, respectively). (2) The contractile effect of 6 beta-AN was inhibited by atropine (1 -100 nmol.L-1) or para-fluoro-hexahydro-sila-difenidol (0.01-1 mumol.L-1), but not by methoctramine (Met, 0.3-3 mumol.L-1) or pirenzepine (0.01-0.1 mumol.L-1), and was not enhanced by tacrine (0.1-10 mumol.L-1) or by epithelium removal. (3) The 6 beta-AN induced-contraction was accompanied by an increase of IP levels in isolated human bronchial tissues. (4) 6 beta-AN had an inhibitory effect on isoprenaline (Iso)-induced relaxation, which was abolished or reduced by Met 0.3 mumol.L-1.

CONCLUSION

6 beta-AN exerts a potent contractile effect involving muscarinic M3 receptor stimulation on airway smooth muscle. Muscarinic M2 receptor stimulation is furthermore partially involved in the antagonism by 6 beta-AN on the Iso-induced relaxation of the guinea pig trachea.

摘要

目的

研究6β-乙酰氧基去甲托烷（6β-AN）对离体人支气管和豚鼠气管的作用。

方法

用4种不同的毒蕈碱受体拮抗剂研究6β-AN的收缩作用，并用放射性流动检测器的高效液相色谱法测定人支气管中肌醇磷酸（IP）的积累。

结果

（1）6β-AN对人支气管的最大收缩作用低于乙酰胆碱（ACh），与ACh对豚鼠气管的作用相当。6β-AN在两种制剂上比ACh更有效（分别为68倍和245倍）。（2）6β-AN的收缩作用被阿托品（1 - 100 nmol·L-1）或对氟六氢硅二苯醚（0.01 - 1 μmol·L-1）抑制，但不被甲溴东莨菪碱（Met，0.3 - 3 μmol·L-1）或哌仑西平（0.01 - 0.1 μmol·L-1）抑制，且不被他克林（0.1 - 10 μmol·L-1）或去除上皮增强。（3）6β-AN诱导的收缩伴随着离体人支气管组织中IP水平的增加。（4）6β-AN对异丙肾上腺素（Iso）诱导的舒张有抑制作用，0.3 μmol·L-1的Met可消除或减弱这种作用。