Biological properties of a new fluorescent biphalin fragment analogue
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- 作者：Lipkowski ; Andrzej W. ; Misicka ; Aleksandra ; Kosson ; Dariusz ; Kosson ; Piotr ; Lachwa-From ; Magdalena ; et. al.
- 关键词：Analgesia ; Opioid peptides ; Fluorescence probe
- 刊名：Life Sciences
- 出版年：2002
- 出版时间：January 11, 2002
- 年：2002
- 卷：70
- 期：8
- 页码：893-897
- 全文大小：99.1 K
文摘
Previous studies of structure-activity of biphalin defined fragments which expressed the full biological potency of the parent compound. The most simple fragment was Tyr-D-Ala-Gly-Phe-NH-NH←X, where X=Phe, but it also could be other hydrophobic amino acids. This paper presents data that replacement of the phenylalanine with a dansyl (X=DNS) groups gives an analogue (AA2016) that fully preserves the high affinity of the initial analogue for both μ and δ opioid receptors. In the tail flick test in rats, intrathecal injection of the compound produces strong antinociception, comparable to the parent biphalin. Because AA2016 contains a strong fluorescent group, it can be a very useful tool for prospective studies in vivo, including biological barrier permeability, tissue distribution, metabolism and receptor-ligand complex formation.