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Reading and Writing the Blood-Brain Barrier: Relevance to Therapeutics

机译:读写血脑屏障:与治疗学的关系

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The blood-brain barrier (BBB) serves to protect the central nervous system (CNS) from damage by exogenous molecules. In doing so, it also can prevent some drugs from reaching their sites of action. Accordingly, a variety of methods for bypassing the BBB have been developed. Ekwuribe et al. recently patented a method for drug conjugation in order to increase lipophilicity, and therefore BBB permeability. Shalev developed a device for opening the barrier via parasympathetic nerve fiber stimulation and Gudkov et al. produced compounds that modulate the activity of multidrug transporter proteins, by either increasing or decreasing the selective permeability of the BBB. A variety of CNS disorders contribute to barrier disruption, and detection of this opening can be used for both diagnostic purposes and for determining time periods when drugs can more easily enter the CNS. While expensive and time-consuming imaging techniques are currently used for this purpose, Janigro et al. have devised a method for detecting plasma levels of S100b, a peripheral protein marker for BBB disruption. These techniques for both "reading" and "writing" the BBB will help new and old medications to reach their pharmacological targets in the CNS.
机译:血脑屏障(BBB)用于保护中枢神经系统(CNS)免受外源分子的损害。这样做还可以防止某些药物到达其作用部位。因此,已经开发出多种绕过BBB的方法。 Ekwuribe等。最近,获得了一种药物结合方法的专利,以增加亲脂性,从而增加BBB的通透性。 Shalev开发了一种通过副交感神经纤维刺激来打开屏障的装置,Gudkov等。通过增加或减少血脑屏障的选择性通透性来生产可调节多药转运蛋白活性的化合物。多种中枢神经系统疾病可导致屏障破坏,检测该开口可用于诊断目的和确定药物更容易进入中枢神经系统的时间段。尽管目前为此目的使用昂贵且费时的成像技术,但Janigro等人(2006年)。已经设计出一种检测血浆S100b水平的方法,S100b是BBB破坏的外周蛋白标志物。这些用于“阅读”和“书写”血脑屏障的技术将帮助新旧药物达到中枢神经系统的药理学目标。

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