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对在豚鼠心肌膜β-肾上腺素能受体上获得的125I标记的3-(4-碘苯氧基)-1-异丙氨基丙-2-醇的结合常数(KD),与其在豚鼠离体心房和气管上获得的解离常数(KB)进行比较。

A comparison of the binding constant (KD) of 125I-labelled 3-(4-iodophenoxy)-1-isopropylamino-propan-2-ol obtained on beta-adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (KB) obtained on guinea-pig isolated atria and trachea.

作者信息

O'Donnell S R, Woodcock E A

出版信息

J Pharm Pharmacol. 1978 Feb;30(2):96-100. doi: 10.1111/j.2042-7158.1978.tb13170.x.

Abstract

The dissociation constant of binding (KD) of 125I-labelled 3-(4-iodophenoxy)-1-isoproplyaminopropan-2-ol (IIP) to guinea-pig myocardial membrane preparations was 2.2 x 10-8M. In pharmacological experiments with the non-labelled material and 60 min contact time, IIP produced a parallel shift in the orciprenaline concentration-response line on guinea-pig isolated tracheal and atrial preparations. The dissociation constant (KB) of IIP was 2.9 x 10-8M on atria (pA2 7.54) and 3.3 x 10-8M on trachea (pA2 7-48). These values indicate that IIP is not a selective beta-adrenoceptor blocking drug. In addition, agreement was found between the affinity constant of this antagonist for beta-adrenoceptors as determined by a direct binding study and an indirect pharmacological study.

摘要

125I标记的3-(4-碘苯氧基)-1-异丙氨基丙-2-醇(IIP)与豚鼠心肌膜制剂的结合解离常数(KD)为2.2×10-8M。在用未标记物质进行的药理学实验中,接触时间为60分钟,IIP使豚鼠离体气管和心房制剂上的奥西那林浓度-反应曲线产生平行位移。IIP在心房上的解离常数(KB)为2.9×10-8M(pA2 7.54),在气管上为3.3×10-8M(pA2 7.48)。这些值表明IIP不是一种选择性β-肾上腺素受体阻断药物。此外,通过直接结合研究和间接药理学研究确定的该拮抗剂对β-肾上腺素受体的亲和力常数之间存在一致性。

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