二甲基苯基哌嗪对大鼠离体膀胱的阿托品样抑制作用。

An atropine-like inhibitory effect of DMPP on rat isolated urinary bladder.

作者信息

Maggi C A, Manzini S, Santicioli P, Meli A

出版信息

J Auton Pharmacol. 1986 Jun;6(2):97-100. doi: 10.1111/j.1474-8673.1986.tb00635.x.

DOI:10.1111/j.1474-8673.1986.tb00635.x

Abstract

DMPP inhibits the nerve-mediated contractions of the rat isolated bladder, its effect being greater in preparations from newborn (2 day old) than adult animals. This effect of DMPP was unaffected by hexamethonium. In preparations from adult animals the effect of DMPP increased with frequency of stimulation and was fully prevented by the presence of atropine. In bladders from newborn rats low concentrations of furthrethonium (FHR) (10 nM) activated a series of rhythmic contractions which were unaffected by tetrodotoxin and abolished by DMPP through an hexamethonium-insensitive action. On the other hand DMPP did not affect rhythmic contractions produced by a low concentration of eledoisin (60 nM). In bladders from adult rats FHR (10 microM) and KCI (30 mM) produced contractures of comparable magnitude. DMPP inhibited, in concentration-related manner the FHR-induced tonic contraction but had little effect on that produced by KCI. These findings indicate that in the rat bladder, DMPP antagonizes selectivity cholinergically-mediated contractions through a mechanism which is unaffected by hexamethonium or tetrodotoxin. An "atropine-like' activity of DMPP should be considered.

摘要

二甲基哌啶磷（DMPP）抑制大鼠离体膀胱的神经介导收缩，其对新生（2日龄）动物标本的作用比对成年动物的作用更强。DMPP的这种作用不受六甲铵的影响。在成年动物的标本中，DMPP的作用随刺激频率增加，且阿托品可完全阻断其作用。在新生大鼠的膀胱中，低浓度的氨甲酰甲胆碱（FHR）（10 nM）可引发一系列节律性收缩，这些收缩不受河豚毒素影响，并可被DMPP通过一种对六甲铵不敏感的作用所消除。另一方面，DMPP不影响低浓度的eledoisin（60 nM）所产生的节律性收缩。在成年大鼠的膀胱中，FHR（10 microM）和氯化钾（30 mM）产生的挛缩程度相当。DMPP以浓度相关的方式抑制FHR诱导的强直性收缩，但对氯化钾产生的收缩影响很小。这些发现表明，在大鼠膀胱中，DMPP通过一种不受六甲铵或河豚毒素影响的机制选择性地拮抗胆碱能介导的收缩。应考虑DMPP具有“阿托品样”活性。