Reinhart P H, Taylor W M, Bygrave F L
Biochem J. 1984 Mar 15;218(3):765-73. doi: 10.1042/bj2180765.
The binding and uptake of [3H]adrenaline by the intact perfused rat liver was investigated. We showed that the administration of [3H]adrenaline to liver resulted in the rapid uptake of the radioligand, and that such uptake was independent of any Ca2+ redistributions induced by the hormone. At low adrenaline concentrations (less than 50 nM) uptake was inhibited by prazosin, whereas at higher hormone concentrations a significant proportion of total [3H]adrenaline uptake could not be inhibited by this antagonist. [3H]Adrenaline uptake could be directly correlated with adrenaline-induced responses such as an increased rate of respiration and glycogenolysis. The partial inhibition (approx. 25%) of [3H]adrenaline uptake by antagonists was sufficient for the total inhibition of hormone-induced responses. The effect of various pharmacological agents on [3H]adrenaline uptake was investigated, and the contribution of tissue-related factors to alpha-adrenergic agonist-antagonist interactions in vivo is discussed.
研究了完整灌注大鼠肝脏对[3H]肾上腺素的结合和摄取情况。我们发现，向肝脏注射[3H]肾上腺素会导致放射性配体的快速摄取，且这种摄取与该激素诱导的任何Ca2+再分布无关。在低肾上腺素浓度（低于50 nM）时，哌唑嗪可抑制摄取，而在较高激素浓度下，总[3H]肾上腺素摄取的很大一部分不能被该拮抗剂抑制。[3H]肾上腺素摄取可与肾上腺素诱导的反应直接相关，如呼吸速率增加和糖原分解。拮抗剂对[3H]肾上腺素摄取的部分抑制（约25%）足以完全抑制激素诱导的反应。研究了各种药理剂对[3H]肾上腺素摄取的影响，并讨论了组织相关因素对体内α-肾上腺素能激动剂-拮抗剂相互作用的作用。
