Facilitation of drug entry into the CNS via transient permeation of blood brain barrier: laboratory and preliminary clinical evidence from bradykinin receptor agonist, Cereport
Facilitation of drug entry into the CNS via transient permeation of blood brain barrier: laboratory and preliminary clinical evidence from bradykinin receptor agonist, Cereport
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DOI：
10.1016/s0361-9230(03)00043-1
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发表时间：
2003-05-15
影响因子：
3.8
通讯作者：
Emerich, DF
中科院分区：
文献类型：
--
作者：
Borlongan, CV;Emerich, DF
一种将药物输送到中枢神经系统（CNS）的新方法涉及激活构成血脑屏障（BBB）的内皮细胞上的受体。最近，选择性B₂缓激肽受体激动剂Cereport（也称为RMP - 7）已被证明可短暂增加血脑屏障的通透性。虽然最初开发是为了增加供应胶质瘤的血管的通透性，但最近的研究表明，Cereport也能增加药物制剂在正常（即非肿瘤）血脑屏障的递送。在这篇综述文章中，我们讨论了卡铂、洛哌丁胺和环孢菌素A向中枢神经系统递送增强的证据，它们分别伴随着化疗、镇痛和神经保护作用的增强。这些观察结果表明，Cereport作为一种辅助疗法用于那些需要药物在中枢神经系统中发挥治疗功效的药物治疗是可行的。因为许多用于中枢神经系统疾病的潜在药物通常不能穿过血脑屏障，所以Cereport诱导的血脑屏障的短暂渗透是一种增强药物治疗的有效策略。（C）2003爱思唯尔科学公司。保留所有权利。
One novel approach of transporting drugs into the central nervous system (CNS) involves the activation of receptors on the endothelial cells comprising the blood brain barrier (BBB). Recently the selective B, bradykinin receptor agonist, Cereport (also called RMP-7), has been shown to transiently increase permeability of the BBB. Although initially developed to increase the permeability of the vasculature feeding glioma, recent studies have demonstrated that Cereport also increases the delivery of pharmacological agents across the normal (i.e. nontumor) BBB. In this review paper, we discuss evidence of enhanced CNS delivery of carboplatin, loperamide, and cyclosporin-A, which are accompanied by enhanced chemotherapeutic, analgesic and neuroprotective effects, respectively. These observations suggest feasibility of Cereport as an adjunct therapy to pharmacological treatments that require drug availability in the CNS to exert therapeutic efficacy. Because many potential drugs for CNS disorders normally do not cross the BBB, Cereport-induced transient permeation of BBB stands as an efficacious strategy for enhancing pharmacotherapy. (C) 2003 Elsevier Science Inc. All rights reserved.