Chemical Biology & Therapeutics group, Department of Experimental Medical Science , Lund University , S-22184 Lund , Sweden.
Division of Clinical Protein Science and Imaging, Department of Experimental Medical Science , Lund University , S-22184 Lund , Sweden.
ACS Chem Neurosci. 2018 Aug 15;9(8):1994-2000. doi: 10.1021/acschemneuro.7b00459. Epub 2018 Jan 19.
Studying how and where drugs are metabolized in the brain is challenging. In an entire organism, peripheral metabolism produces many of the same metabolites as those in the brain, and many of these metabolites can cross the blood-brain barrier from the periphery, thus making the relative contributions of hepatic and brain metabolism difficult to study in vivo. In addition, drugs and metabolites contained in ventricles and in the residual blood of capillaries in the brain may overestimate drugs' and metabolites' concentrations in the brain. In this study, we examine locusts and zebrafish using matrix assisted laser desorption ionization mass spectrometry imaging to study brain metabolism and distribution. These animal models are cost-effective and ethically sound for initial drug development studies.
研究药物在大脑中的代谢途径和位置具有挑战性。在完整的生物体中,外周代谢会产生许多与大脑中相同的代谢物,而且其中许多代谢物可以从外周穿过血脑屏障,从而使得肝代谢和脑代谢的相对贡献难以在体内进行研究。此外,脑室中的药物和代谢物以及脑毛细血管中残留血液中的药物和代谢物可能会高估脑内药物和代谢物的浓度。在这项研究中,我们使用基质辅助激光解吸电离质谱成像技术研究了蝗虫和斑马鱼的大脑代谢和分布,这些动物模型在药物开发的初步研究中具有成本效益和伦理优势。