Wellstein A, Jablonka B, Wiemer G, Palm D
Pol J Pharmacol Pharm. 1984 Mar-Jun;36(2-3):265-73.
After treatment of rats with 5 x 0.5 mg/kg/d reserpine in membrane preparations from the parotid gland no increase in the total number of beta-adrenoceptors (Bmax) was observed using the antagonist ligand (-)3H-dihydroalprenolol. There occurred, however, a pronounced increase of the high affinity agonist binding component. Thus, it appears that not the absolute number of beta-adrenoceptor sites but the relative amount of high affinity sites is most sensitive against the sensitization process. The results are in contrast to those of other authors. We suspect that increases of Bmax-values after reserpine can be simulated by the loss of noradrenaline whereas in control membranes noradrenaline is still bound to the adrenoceptors thus preventing the radioactive ligand from access to these sites. We highly recommend to use preincubation methods prior to ligand binding studies in order to remove endogenous ligands still bound to the high affinity site of the beta-adrenoceptor.
用5×0.5毫克/千克/天的利血平处理大鼠后,在腮腺膜制剂中,使用拮抗剂配体(-)3H-二氢阿普洛尔未观察到β-肾上腺素能受体总数(Bmax)增加。然而,高亲和力激动剂结合成分出现了明显增加。因此,似乎对致敏过程最敏感的不是β-肾上腺素能受体位点的绝对数量,而是高亲和力位点的相对数量。这些结果与其他作者的结果相反。我们怀疑利血平后Bmax值的增加可以通过去甲肾上腺素的丧失来模拟,而在对照膜中,去甲肾上腺素仍与肾上腺素能受体结合,从而阻止放射性配体接近这些位点。我们强烈建议在配体结合研究之前使用预孵育方法,以去除仍与β-肾上腺素能受体高亲和力位点结合的内源性配体。