Gaining insights into the pharmacokinetic and pharmacodynamic properties of lead compounds is crucial during drug development processes. When it comes to the treatment of brain diseases, collecting information at the site of action is challenging. There are only a few techniques available that allow for the direct sampling from the cerebral interstitial space. This review concerns the applicability of microdialysis and other approaches, such as cerebral open flow microperfusion and electrochemical biosensors, to monitor macromolecules (neuropeptides, proteins, …) in the brain. Microdialysis and cerebral open flow microperfusion can also be used to locally apply molecules at the same time at the site of sampling. Innovations in the field are discussed, together with the pitfalls. Moreover, the ‘nuts and bolts’ of the techniques and the current research gaps are addressed. The implementation of these techniques could help to improve drug development of brain-targeted drugs.

中文翻译：

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目前直接从脑组织液中监测大分子的方法

深入了解先导化合物的药代动力学和药效学特性在药物开发过程中至关重要。在治疗脑部疾病时，在作用部位收集信息具有挑战性。只有少数几种技术可以直接从脑间质空间取样。本综述涉及微透析和其他方法（如脑开流微灌注和电化学生物传感器）在监测大脑中大分子（神经肽、蛋白质等）的适用性。微透析和脑开流微灌注也可用于在取样部位同时局部应用分子。讨论了该领域的创新以及陷阱。而且，解决了技术的“基本要素”和当前的研究差距。这些技术的实施可能有助于改善脑靶向药物的药物开发。