Zhao S J, Sun G L, Cao Y S
Department of Pharmacology, He-nan Medical University, Zhengzhou, China.
Zhongguo Yao Li Xue Bao. 1990 May;11(3):210-3.
Pretreatment to guinea pigs with sc isoprenaline (Iso) 10 micrograms/kg tid x 7 d reduced the effect of Iso on protecting histamine-induced asthma and decreased its pD2 values in relaxing isolated tracheal strip. This treatment did not change the asthmatic effect induced by histamine and the effect of Iso on positive chronotropic action, but elevated the blood pressure. These results suggest that it is easier to develop the tolerance of beta 2-adrenoceptors of respiratory smooth muscles than that of beta 1-adrenoceptors of heart. Radioligand binding assay showed that the treatment decreased the number of binding sites of beta-adrenoceptors on lungs of guinea pigs but did not change the binding affinity.
对豚鼠皮下注射异丙肾上腺素(Iso)10微克/千克,每日3次,共7天进行预处理,可降低Iso对组胺诱导的哮喘的保护作用,并降低其在舒张离体气管条时的pD2值。这种处理并未改变组胺诱导的哮喘效应以及Iso对正性变时作用的效应,但会使血压升高。这些结果表明,呼吸道平滑肌的β2 -肾上腺素能受体比心脏的β1 -肾上腺素能受体更容易产生耐受性。放射性配体结合试验表明,该处理可减少豚鼠肺组织中β -肾上腺素能受体的结合位点数量,但不改变结合亲和力。