NPFFR1 Membrane Protein Introduction

Introduction of NPFFR1

Neuropeptide FF receptor 1 (NPFFR1), also known as NPFF1, is the human protein encoded by the NPFFR1 gene. NPFF is the endogenous octapeptide membrane belongs to the family of neuropeptides which display a conserved Arg-Phe-NH₂ at the C-terminal end. The NPFF can be detected in periaqueductal gray, dorsal spinal cord, medulla pons, and the hypothalamus with high concentrations. NPFF1 and NPFF2 are two G protein-coupled receptors isolated from human central nervous system issues and the expression level of NPFFR1 mRNA is higher in the central nervous system (CNS) than in peripheral tissues.

Basic Information of NPFFR1
Protein Name	Neuropeptide FF receptor 1
Gene Name	NPFFR1
Aliases	NPFF1, GPR147, NPFF1R1, OT7T022
Organism	Homo sapiens (Human)
UniProt ID	Q9GZQ6
Transmembrane Times	7
Length (aa)	430
Sequence	MEGEPSQPPNSSWPLSQNGTNTEATPATNLTFSSYYQHTSPVAAMFIVAYALIFLLCMVGNTLVCFIVLKNRHMHTVTNMFILNLAVSDLLVGIFCMPTTLVDNLITGWPFDNATCKMSGLVQGMSVSASVFTLVAIAVERFRCIVHPFREKLTLRKALVTIAVIWALALLIMCPSAVTLTVTREEHHFMVDARNRSYPLYSCWEAWPEKGMRRVYTTVLFSHIYLAPLALIVVMYARIARKLCQAPGPAPGGEEAADPRASRRRARVVHMLVMVALFFTLSWLPLWALLLLIDYGQLSAPQLHLVTVYAFPFAHWLAFFNSSANPIIYGYFNENFRRGFQAAFRARLCPRPSGSHKEAYSERPGGLLHRRVFVVVRPSDSGLPSESGPSSGAPRPGRLPLRNGRVAHHGLPREGPGCSHLPLTIPAWDI

Function of NPFFR1 Membrane Protein

As opiate tolerance and dependence are major clinical and social problems, the neuropeptide FF isolated from the human central nervous system is believed to be implicated in pain modulation as well as opiate tolerance and plays an important role in these processes. Some studies also have shown that NPFF is involved in various physiological processes, including food intake, blood pressure regulation, insulin release, memory, and electrolyte balance. In addition, NPFF presents both anti-opioid and pro-opioid actions in different animal models of pain, although its exact mechanism is currently unknown. The research suggesting that NPFF elicits its actions through a G protein-coupled receptor, which can specifically bind and be activated by NPFF and the related peptides.

Fig.1 Subcellular location of NPFFR1.

Application of NPFFR1 Membrane Protein in Literature

Hammoud H., et al. Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid-induced hyperalgesia. Acs Chemical Neuroscience. 2018. PubMed ID: 29727163

NPFFR1, NPFFR2, and their endogenous ligand NPFF present anti-opioid properties and play important roles in the adverse effects. Authors in this group seek to identify the novel NPFF receptor ligands based on a series of heterocycles as rigidified non-peptide NPFF receptor ligands.
Drieu A.L.R., et al. A bifunctional biased mu-opioid agonist - neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects. Pain. 2018. PubMed ID: 29708942

NPFF and its receptors (NPFF1R and NPFF2R) have been served as an important pronociceptive system involved in analgesic tolerance and opioid-induced hyperalgesia. This article gives a strategy which leads to the development of novel and potent antinociceptive drugs.
Thorson J.F., et al. Relationship of neuropeptide FF receptors with pubertal maturation of gilts. Biology of Reproduction. 2017, 96(3): 617-634. PubMed ID: 28339619

This article reveals that there is an RFFP system in the pig and NPFFR2 is important for pubertal onset in gifts. The mechanism is still unclear now.
Wang Z.L., et al. Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities. Journal of Medicinal Chemistry. 2016, 59(22): 10198-10208. PubMed ID: 27798836

This article reveals that it is reasonable to produce effective nontolerance forming antinociception when designing the multifunctional peptide ligands for opioid and NPFF receptors in a single molecule.
Bihel F., et al. Development of a Peptidomimetic Antagonist of Neuropeptide FF Receptors for the Prevention of Opioid-Induced Hyperalgesia. Acs Chemical Neuroscience. 2015, 6(3): 438. PubMed ID: 25588572

This article designs an orally active peptidomimetic antagonist of NPFFR which can potentiate the opioid-induced analgesia. This derivative provides a novel therapeutic approach to improve analgesia and reduce hyperalgesia.

NPFFR1 Preparation Options

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