Goldstein A, Nestor J J, Naidu A, Newman S R
Department of Pharmacology, Stanford University, CA 94305.
Proc Natl Acad Sci U S A. 1988 Oct;85(19):7375-9. doi: 10.1073/pnas.85.19.7375.
We describe a synthetic ligand, "DAKLI" (Dynorphin A-analogue Kappa LIgand), related to the opioid peptide dynorphin A. A single reactive amino group at the extended carboxyl terminus permits various reporter groups to be attached, such as 125I-labeled Bolton-Hunter reagent, fluorescein isothiocyanate, or biotin. These derivatives have high affinity and selectivity for the dynorphin (kappa opioid) receptor. An incidental finding is that untreated guinea pig brain membranes have saturable avidin binding sites.
我们描述了一种与阿片肽强啡肽A相关的合成配体“DAKLI”(强啡肽A类似物κ配体)。在延长的羧基末端的单个反应性氨基允许连接各种报告基团,如125I标记的博尔顿-亨特试剂、异硫氰酸荧光素或生物素。这些衍生物对强啡肽(κ阿片样物质)受体具有高亲和力和选择性。一个偶然的发现是未处理的豚鼠脑膜具有可饱和的抗生物素蛋白结合位点。