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非诺特罗和沙丁胺醇对豚鼠子宫肌层的作用:卵巢甾体激素的影响。

Fenoterol and salbutamol actions on guinea-pig myometrium: effects of ovarian steroids.

作者信息

Mammen G J, Handberg G M, Story M E, Pennefather J N

机构信息

Department of Pharmacology, Monash University, Clayton, Victoria, Australia.

出版信息

Eur J Pharmacol. 1987 Nov 10;143(2):229-35. doi: 10.1016/0014-2999(87)90537-1.

Abstract

Responses of isolated preparations of longitudinal myometrium from the guinea-pig to fenoterol, salbutamol and isoprenaline were examined. Virgin adult guinea-pigs were treated (i) with oestradiol cypionate 20 micrograms/kg s.c. thrice weekly for two weeks; or (ii) as in (i) plus progesterone 3 mg/animal for the last four days. Other animals (diestrous; cycle days 6-10) were untreated. The order of potency of the agonists in inhibiting field stimulation-induced contractions of the preparations (isoprenaline greater than or equal to fenoterol greater than salbutamol) indicated interaction with beta 2-adrenoceptors. Oestrogen treatment enhanced the potency of isoprenaline 5-fold. Treatment with oestrogen plus progesterone enhanced the potency of all agonists 10- to 30-fold, and increased the mean maximum response to salbutamol. The mean pKD values for displacement by fenoterol of binding of (-)-[125I]cyanopindolol to membrane preparations from animals in both treatment groups were 5.57-5.92. These results raise the possibility that progesterone may enhance the coupling of beta 2-adrenoceptors to transduction mechanisms in the longitudinal myometrium from oestrogen-primed guinea-pigs.

摘要

研究了豚鼠离体纵行子宫肌层制剂对非诺特罗、沙丁胺醇和异丙肾上腺素的反应。成年未孕豚鼠接受如下处理:(i)皮下注射环戊丙酸雌二醇20微克/千克,每周3次,共2周;或(ii)按(i)处理,在最后4天加用黄体酮3毫克/只动物。其他动物(动情后期;周期第6 - 10天)未作处理。激动剂抑制制剂的场刺激诱导收缩的效价顺序(异丙肾上腺素≥非诺特罗>沙丁胺醇)表明其与β2 - 肾上腺素受体相互作用。雌激素处理使异丙肾上腺素的效价增强5倍。雌激素加黄体酮处理使所有激动剂的效价增强10至30倍,并增加了对沙丁胺醇的平均最大反应。两个处理组动物的膜制剂中,非诺特罗置换( - ) - [125I]氰基吲哚洛尔结合的平均pKD值为5.57 - 5.92。这些结果提示,黄体酮可能增强雌激素预处理的豚鼠纵行子宫肌层中β2 - 肾上腺素受体与转导机制的偶联。

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