公开(公告)号：US06258780B1

公开(公告)日：2001-07-10

申请号：US08975084

申请日：1997-11-20

申请人： Hermona Soreq ,  Alon Friedman ,  Shlomo Siedman ,  Daniela Kaufer

发明人： Hermona Soreq ,  Alon Friedman ,  Shlomo Siedman ,  Daniela Kaufer

IPC分类号： A61K3816

CPC分类号： C12Y301/01007 ,  A61K31/137 ,  A61K31/138 ,  A61K31/46 ,  A61K38/465 ,  A61K2300/00

摘要： A pharmaceutical composition for facilitating passage of compounds through the blood-brain barrier comprising the agent ACHE-I4 readthrough (SEQ ID No:1) splice variant or the I4 peptide (SEQ ID No:2) and analogues of each thereof and a pharmaceutically acceptable carrier is disclosed. Alternatively, the pharmaceutical composition for facilitating passage of compounds through the blood-brain barrier can comprise the agents adrenaline, atropine, dopamine and/or an adrenergic combination and a pharmaceutically acceptable carrier. The composition can comprise at least two of the agents. The composition of the present invention can optionally include the compound to be transported across the blood-brain barrier. Alternatively, the compound can be co-administered (simultaneously) with the composition or can be administered at some point during the biologically effective period of the action of the composition. The present invention provides a method for administering a compound to the CNS of an animal by subjecting the animal to a stress-mimicking agent or treatment. This agent or treatment facilitates disruption of the blood-brain barrier. During the period that the BBB is opened or disrupted a compound can be administer such that the compound is enabled to passage through the disrupted BBB into the CNS.

摘要翻译： 一种用于促进化合物通过包含透明试剂ACHE-I4（SEQ ID No：1）剪接变体或I4肽（SEQ ID No：2）及其各自的类似物的药物组合物和药学上可接受的药物组合物 载体被披露。 或者，用于促进化合物通过血脑屏障的药物组合物可以包含肾上腺素，阿托品，多巴胺和/或肾上腺素能组合剂和药学上可接受的载体。 所述组合物可包含至少两种所述试剂。 本发明的组合物可以任选地包括待跨越血脑屏障转运的化合物。 或者，化合物可以与组合物共同施用（同时），或者可以在组合物的作用的生物学有效期间的某一点施用。 本发明提供了通过使动物经受应激模拟剂或治疗而将化合物给予动物的CNS的方法。 该药剂或治疗有助于破坏血脑屏障。 在BBB开放或中断期间，可以给予化合物使得化合物能够通过破坏的BBB进入CNS。