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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.

DOI:10.1111/j.1440-1681.1978.tb00689.x
PMID:699383
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。

相似文献

1
Agonistic and antagonistic actions of 3,4-dihydroxy-substituted phenoxypropanolamines in guinea-pig atria and trachea.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。
Clin Exp Pharmacol Physiol. 1978 Jul-Aug;5(4):393-8. doi: 10.1111/j.1440-1681.1978.tb00689.x.
2
Catechol-substituted phenoxypropanolamines: adrenoceptor activity in the anaesthetized cat.儿茶酚取代的苯氧基丙醇胺:麻醉猫中的肾上腺素能受体活性
Br J Pharmacol. 1977 Jun;60(2):197-203. doi: 10.1111/j.1476-5381.1977.tb07741.x.
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Phenoxypropanolamines as selective beta 1-receptor agonists.
Circ Res. 1980 Jun;46(6 Pt 2):I53-4.
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Beta-adrenoceptor subtypes and the opening of plasmalemmal K(+)-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue.β-肾上腺素能受体亚型与气管平滑肌中质膜钾通道的开放:豚鼠组织的电生理和力学研究
Br J Pharmacol. 1993 Aug;109(4):1140-8. doi: 10.1111/j.1476-5381.1993.tb13741.x.
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Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency.心肌β1-肾上腺素能受体的直接标记。3H-(-)-比索洛尔结合亲和力与其阻断效能的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Oct;331(1):27-39. doi: 10.1007/BF00498849.
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Relaxation of cat trachea by beta-adrenoceptor agonists can be mediated by both beta1- and beta2-adrenoceptors and potentiated by inhibitors of extraneuronal uptake.β-肾上腺素能激动剂对猫气管的舒张作用可由β1-和β2-肾上腺素能受体介导,并可被非神经元摄取抑制剂增强。
Br J Pharmacol. 1983 Feb;78(2):417-24. doi: 10.1111/j.1476-5381.1983.tb09406.x.
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The beta-adrenoceptor stimulant properties of OPC-2009 on guinea-pig isolated tracheal, right atrial and left atrial preparations.OPC - 2009对豚鼠离体气管、右心房和左心房标本的β - 肾上腺素能受体刺激特性。
Br J Pharmacol. 1977 Dec;61(4):513-21. doi: 10.1111/j.1476-5381.1977.tb07543.x.
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Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol.环丙洛尔、扎莫特罗和吲哚洛尔对β-1肾上腺素能受体激动剂及拮抗剂效能和选择性的比较分析
J Pharmacol Exp Ther. 1987 Sep;242(3):1025-34.
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Functional properties of atypical beta-adrenoceptors on the guinea pig duodenum.豚鼠十二指肠非典型β-肾上腺素能受体的功能特性
Eur J Pharmacol. 2001 Mar 23;416(1-2):153-63. doi: 10.1016/s0014-2999(01)00877-9.
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The use of functional antagonism to determine whether beta-adrenoceptor agonists must have a lower efficacy than isoprenaline to be trachea-atria selective in vitro in guinea-pigs.利用功能拮抗作用来确定β-肾上腺素能受体激动剂在豚鼠体外实验中对气管-心房具有选择性时,其效能是否必定低于异丙肾上腺素。
Br J Pharmacol. 1977 Jun;60(2):255-62. doi: 10.1111/j.1476-5381.1977.tb07748.x.

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In vitro activity of RO363, a beta1-adrenoceptor selective agonist.β1肾上腺素能受体选择性激动剂RO363的体外活性
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