Halper J P, Mann J J, Weksler M E, Bilezikian J P, Sweeney J A, Brown R P, Golbourne T
Life Sci. 1984 Aug 20;35(8):855-63. doi: 10.1016/0024-3205(84)90411-9.
A saturable, stereospecific high affinity beta 2 adrenergic receptor was demonstrated on intact human peripheral blood lymphocytes using the ligand [125I]-iodocyanopindolol ([125I]ICYP). A method is described for parallel measurements of saturation binding isotherms and isoproterenol-cAMP responsiveness in split samples of intact lymphocytes isolated from 40 ml. of whole blood. A significant positive correlation between beta receptor density (Bmax) and the ratio of maximal isoproterenol-generated cAMP to basal levels was found in healthy subjects (r = 0.65, p less than 0.001). A significant positive correlation was found between age and the fold increase over basal cAMP levels induced by isoproterenol. Older females had a significantly higher fold increase in cAMP levels after isoproterenol than older males. These effects were largely accounted for by the lower basal levels of cAMP in older subjects. Beta receptor binding indices (Bmax and KD) did not differ between males and females, or change with aging. The effects of age and sex upon cAMP levels appear to be at least partly mediated by mechanisms independent of the beta receptor. The method, which describes a convenient assay for parallel measurement of beta receptor binding and cAMP levels in small blood samples, represents a useful model for studying human beta receptor function.
利用配体[125I] - 碘氰吲哚洛尔([125I]ICYP)在完整的人外周血淋巴细胞上证实了一种可饱和、立体特异性的高亲和力β2肾上腺素能受体。本文描述了一种方法,用于对从40毫升全血中分离出的完整淋巴细胞的分割样本进行饱和结合等温线和平行测量异丙肾上腺素 - cAMP反应性。在健康受试者中发现β受体密度(Bmax)与最大异丙肾上腺素生成的cAMP与基础水平的比值之间存在显著正相关(r = 0.65,p < 0.001)。发现年龄与异丙肾上腺素诱导的基础cAMP水平的增加倍数之间存在显著正相关。老年女性在使用异丙肾上腺素后cAMP水平的增加倍数明显高于老年男性。这些影响在很大程度上是由于老年受试者中较低的基础cAMP水平。β受体结合指数(Bmax和KD)在男性和女性之间没有差异,也不会随年龄变化。年龄和性别对cAMP水平的影响似乎至少部分是由独立于β受体的机制介导的。该方法描述了一种方便的检测方法,用于在小血样中平行测量β受体结合和cAMP水平,是研究人β受体功能的有用模型。