【摘要】 生物胺转运体(BAT)是生物膜上的一种蛋白质,它通过将底物从细胞外转运到神经末端来终止多巴胺(DA)、5-羟色胺(5-HT)和去甲肾上腺素(NE)的作用。大量药物和给药方法以BAT为靶点,以底物或抑制剂的形式发挥作用。本文总结了作用于BAT上的药物活性的几种测量方法,并以麻黄碱及其立体异构体为例来讨论这些方法用来发现天然活性物质的潜在应用。更多还原

【Abstract】 Biogenic amine transporters(BATs) are integral membrane proteins that terminate the actions of dopamine(DA),serotonin(5-HT) and norepinephrine(NE) by pumping these substrates from the extracellular space back into the nerve terminal.Numerous drugs and medications target BATs,acting as inhibitors or substrates.This paper reviews some of the methods used to measure the activity of test drugs at the BATs.These methods include traditional uptake inhibition assays and transporter binding assays,as well as methods to determine if a test agent is a BAT substrate or inhibitor.The potential application of these methods for characterizing natural products will be discussed in reference to results obtained with "purified" natural products,such as ephedrine stereoisomers.更多还原