Department of Medicinal Chemistry, 419 Faser Hall, The University of Mississippi, MS 38677, USA.
Future Med Chem. 2012 Jun;4(9):1085-92. doi: 10.4155/fmc.12.67.
Neuropeptide FF (NPFF) was first isolated from the bovine brain in 1985 and is linked with a variety of biological activities. NPFF, which belongs to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2). These receptors are distributed throughout the body. The NPFF system was initially described as an anti-opioid system and, while the NPFF system does affect the opioid system, it also has been implicated in pain modulation, changes in arterial blood pressure, feeding behavior and regulation of core body temperature and of monoamine systems. Most of this pharmacology has been realized from the peptide NPFF itself or through peptide analogs. The quest for nonpeptide tools for this receptor system has been limited by low selectivity and poor pharmacokinetic properties. Herein, we summarize the current knowledge from the scientific and patent literature that demonstrates a clear need for future medicinal chemistry efforts.
神经肽 FF（NPFF）于 1985 年首次从牛脑中分离出来，与多种生物活性有关。NPFF 属于 RF-酰胺肽家族，与两种不同的 G 蛋白偶联受体 NPFF(1)和 NPFF(2)相互作用。这些受体分布在全身。NPFF 系统最初被描述为一种抗阿片系统，虽然 NPFF 系统确实会影响阿片系统，但它也与疼痛调节、动脉血压变化、进食行为以及核心体温和单胺系统的调节有关。这些药理学大部分是通过肽 NPFF 本身或通过肽类似物来实现的。由于低选择性和差的药代动力学特性，针对该受体系统的非肽工具的探索受到限制。本文综述了来自科学和专利文献的现有知识，表明未来需要进行药物化学研究。
