大鼠子宫平滑肌中组胺快速耐受性的特征

Characteristics of histamine tachyphylaxis in rat uterine smooth muscle.

作者信息

Martínez-Mir I, Gil Marqués M, Morales-Olivas F J, Rubio-Gomis E

机构信息

Departament de Farmacologia, Universitat de València, Spain.

出版信息

Inflamm Res. 2002 Dec;51(12):587-93. doi: 10.1007/pl00012433.

DOI:10.1007/pl00012433

PMID:12558192

Abstract

OBJECTIVE AND DESIGN

To study both the desensitisation induced by short-term exposure to histamine and the mechanism responsible in the isolated rat uterus.

MATERIAL

Precontracted isolated uterus (37 mM KCl) from oestrogenised Wistar rats were used.

TREATMENT

Repetitive responses to histamine (10(-6), 10(-5), 10(-4), 10(-3) M), dimaprit and clonidine (10(-4) M) were tested at 15, 30, 45 and 105 min., with their modifications by (5 mg/kg, 24 h before sacrifice) reserpine, 10(-7) M propranolol, 10(-8) M atropine, and 10(-6) M indomethacin. Dose-response curves for adrenaline were carried out as standard protocol.

METHODS

In vitro techniques (de Jalon's solution, 31 degrees C, carbogen, isotonic registration, resting tension 1 g). Levels of cAMP were studied in response to histamine, adrenaline and isoproterenol by radioassay.

RESULTS

Repeated histamine produced a rapid loss of inhibitory uterine response depending on the number of exposures and increase in concentration. The tachyphylaxis phenomenon is not modified by the different pretreatments used. Dimaprit, but not clonidine or adrenaline, produced tachyphylaxis. The second exposition to 10(-3) M histamine produced a 38.8% reduction in cAMP production.

CONCLUSION

Histamine appears to induce homologous and probably cAMP-dependent desensitisation of H2-receptors.

摘要

目的与设计

研究短期暴露于组胺所诱导的脱敏作用及其在离体大鼠子宫中的作用机制。

材料

使用来自经雌激素处理的Wistar大鼠的预收缩离体子宫（37 mM氯化钾）。

处理

在15、30、45和105分钟时测试对组胺（10⁻⁶、10⁻⁵、10⁻⁴、10⁻³ M）、地马普明和可乐定（10⁻⁴ M）的重复反应，以及它们在（处死前24小时5 mg/kg）利血平、10⁻⁷ M普萘洛尔、10⁻⁸ M阿托品和10⁻⁶ M吲哚美辛作用下的变化。按照标准方案进行肾上腺素的剂量-反应曲线测定。