连接子取代对丁丙诺啡单价和双价配体与阿片受体结合的影响。
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
机构信息
Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. doi: 10.1016/j.bmcl.2010.01.101. Epub 2010 Jan 25.
Abstract
A series of bivalent hydroxy ether butorphan ligands were prepared and their binding affinities at the opioid receptors determined. Addition of a hydroxy group to a hydrocarbon chain can potentiate binding affinity up to 27- and 86-fold at the mu and kappa opioid receptors, respectively. Two bivalent ligands with sub-nanomolar binding affinity at the mu and kappa opioid receptors were discovered.
摘要
制备了一系列二价羟乙醚丁丙诺啡配体，并测定了它们在阿片受体上的结合亲和力。在烃链上添加一个羟基可以使μ和κ阿片受体的结合亲和力分别增强 27 倍和 86 倍。发现了两种具有亚纳摩尔结合亲和力的二价配体，分别在μ和κ阿片受体上。
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