Tyacke Robin J, Nutt David J
Centre for Neuropsychopharmacology, Division of Brain Sciences, Hammersmith Hospital, Imperial College London, W12 0NN, United Kingdom.
Synapse. 2015 Oct;69(10):505-11. doi: 10.1002/syn.21835. Epub 2015 Jul 14.
A major goal in neuroscience is the measurement of neurotransmitters in living human brain. To date this has only been done reliably with dopamine using certain PET and SPECT radiotracers. The use of this technique has greatly advanced our understanding of dopamine and the dopaminergic system in normal and abnormal brain function. Transferring this technology to other neurotransmitter systems has proved less fruitful. The serotonergic system (5-HT) is one such system. 5-HT has been implicated in a wide range of brain functions and their disorders. The ability to measure 5-HT using this technique would be invaluable. In this article, we explore the key pharmacological features of current radiotracers for 5-HT receptors that might be sensitive to endogenous 5-HT. We also estimate the likely brain concentrations of the current available tranche of agents that might be used to enhance synaptic 5-HT concentration, so taking into account the potential for these to interact with the receptors directly and produce a spurious displacement signal.
神经科学的一个主要目标是测量活体人类大脑中的神经递质。迄今为止，只有使用某些正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）放射性示踪剂对多巴胺进行测量时才具有可靠性。这项技术的应用极大地推动了我们对多巴胺以及多巴胺能系统在正常和异常脑功能中的理解。事实证明，将这项技术应用于其他神经递质系统的成效较小。血清素能系统（5-羟色胺，5-HT）就是这样一个系统。5-HT与多种脑功能及其紊乱有关。利用这项技术测量5-HT的能力将非常宝贵。在本文中,我们探讨了当前对内源性5-HT可能敏感的5-HT受体放射性示踪剂的关键药理学特征。我们还估计了当前可用的、可能用于提高突触5-HT浓度的药物在大脑中的可能浓度，从而考虑到这些药物直接与受体相互作用并产生虚假置换信号的可能性。
