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对马和人尿液以及马血浆中的17种 Dermorphin 肽进行高通量筛选。

A high throughput screen for 17 Dermorphin peptides in equine and human urine and equine plasma.

作者信息

Steel Rohan, Timms Mark, Levina Vita, Vine John

机构信息

Biological Research Unit, Racing Analytical Services Ltd, 400 Epsom Road, Flemington, Victoria, Australia, 3031.

出版信息

Drug Test Anal. 2014 Sep;6(9):909-21. doi: 10.1002/dta.1585. Epub 2013 Nov 20.

DOI:10.1002/dta.1585
PMID:24259424
Abstract

The Dermorphins are a family of peptides that act as potent agonists of the opioid μ receptor. Originally identified as a seven amino acid peptide on the skin of the South American Phyllomedusa frog, peptide chemists have since developed a large number of Dermorphin variants, many with superior opioid activity to the original peptide. Dermorphins are unique among the peptide opioid agonists as they appear to have a limited ability to cross the blood brain barrier, producing effects on both the central and peripheral nervous systems. It is this ability of Dermorphins to provide central anaesthesia after intravenous or subcutaneous administration that allows their use as analogues of the opioid class of drugs. Recently, illicit use of the Dermorphin peptide in the racing industry has shown the need for an analytical method to control the use of these peptides. We present a high-throughput liquid chromatography-tandem mass spectrometry screen for 17 Dermorphin peptides in equine urine and plasma with limits of detection down to 5 pg/mL. The peptide extraction technique is also suitable for use in human urine.

摘要

德尔吗啡肽是一类作为阿片μ受体强效激动剂的肽。最初在南美洲叶泡蛙的皮肤中被鉴定为一种七肽,此后肽化学家们开发了大量的德尔吗啡肽变体,其中许多变体的阿片活性优于原始肽。德尔吗啡肽在肽类阿片激动剂中是独特的,因为它们穿越血脑屏障的能力似乎有限,会对中枢和外周神经系统产生影响。正是德尔吗啡肽在静脉或皮下给药后提供中枢麻醉的这种能力,使其能够用作阿片类药物的类似物。最近,赛马行业中非法使用德尔吗啡肽表明需要一种分析方法来控制这些肽的使用。我们展示了一种用于马尿和血浆中17种德尔吗啡肽的高通量液相色谱 - 串联质谱筛查方法,检测限低至5 pg/mL。该肽提取技术也适用于人尿。

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