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3,4-二羟基取代苯氧基丙醇胺在豚鼠心房和气管中的激动和拮抗作用。

Agonistic and antagonistic actions of 3,4-dihydroxy-substituted phenoxypropanolamines in guinea-pig atria and trachea.

作者信息

Keh G S, Raper C, Dowd H

出版信息

Clin Exp Pharmacol Physiol. 1978 Jul-Aug;5(4):393-8. doi: 10.1111/j.1440-1681.1978.tb00689.x.

Abstract
  1. Racemic mixtures of noradrenaline, adrenaline, isoprenaline, N-t-butylnor-adrenaline and their corresponding derivatives containing an oxymethylene (OM) link between the phenyl ring and ethanolamine side-chain have been tested for their effects on beta-adrenoceptors in isolated guinea-pig atrial and tracheal preparations. 2. In atrial and in spontaneously contracted tracheal preparations both the parent catecholamines and their corresponding OM-derivatives had a similar order of potency as beta-receptor agonists. 3. In carbachol-stimulated tracheal preparations the OM-derivatives were shown to have partial agonistic actions. 4. As in other phenylethanolamines and phenoxypropanolamines, both the agonistic and antagonistic potency of the OM-derivatives increased with increasing amine substitution.
摘要
  1. 已对去甲肾上腺素、肾上腺素、异丙肾上腺素、N-叔丁基去甲肾上腺素的外消旋混合物及其在苯环与乙醇胺侧链之间含有羟亚甲基(OM)连接的相应衍生物,在离体豚鼠心房和气管制剂中对β-肾上腺素能受体的作用进行了测试。2. 在心房和自发收缩的气管制剂中,母体儿茶酚胺及其相应的OM-衍生物作为β-受体激动剂具有相似的效价顺序。3. 在卡巴胆碱刺激的气管制剂中,OM-衍生物表现出部分激动作用。4. 与其他苯乙醇胺和苯氧丙醇胺一样,OM-衍生物的激动和拮抗效价均随胺取代度的增加而增加。

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