Casadó V, Mallol J, Franco R, Lluis C, Canela E I
Departament de Bioquímica i Fisiologia, Facultat de Química, Universitat de Barcelona, Catalonia, Spain.
Naunyn Schmiedebergs Arch Pharmacol. 1994 May;349(5):485-91. doi: 10.1007/BF00169137.
The results described in this paper show, for the first time, that A1 adenosine receptors can have two kinetic components for the binding of the antagonist [3H]DPCPX. At low ionic strength (< or = 42 mmol/l), dissociation of [3H]DPCPX bound to A1 receptors fitted better to a two kinetic components model than to a one kinetic component model. The kinetic constants were consistent with comparable Kd values for the two components of the antagonist binding, and therefore these two components cannot be distinguished by saturation isotherm analysis.
本文所述结果首次表明,A1腺苷受体对于拮抗剂[3H]DPCPX的结合可具有两个动力学组分。在低离子强度(≤42 mmol/l)下,与A1受体结合的[3H]DPCPX的解离更符合双动力学组分模型而非单动力学组分模型。动力学常数与拮抗剂结合的两个组分的可比Kd值一致,因此这两个组分无法通过饱和等温线分析加以区分。