Neuropeptide FF GPCR Assays
Background of Neuropeptide FF Receptors
Neuropeptide FF receptors (NMFFRs), consisting of NPFF-R1 and NPFF-R2, represent two members of the GPCR superfamily. The research on NMFFR and its ligands Neuropeptide FF and Neuropeptide AF can contribute to the development of analgesic drugs and epilepsy treatment, etc.
Fig.1. Structure of the mice Neuropeptide FF receptor 1. (Uniprot ID E9Q468; obtained from Alphafold)
Distribution and Function of Neuropeptide FF Receptors
NPFF receptors are mainly detected in the cerebral cortex region, hypothalamus area, spinal cord, and brainstem, in recent years it has also been found to be expressed in the limbic system. NMFFRs mainly affect the neuroendocrine function, neuropeptide secretion, and perception of pain in mammals, and also play a certain role in the resistance and withdrawal reaction generated by analgesic drugs like morphine and other opioids.
Subtypes and Mechanisms of Neuropeptide FF Receptors
NPFF-R1 and NPFF-R2 can be bound and activated by four different types of peptides and initiate similar effects.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| NPFF-R1 | GPR147 |
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NPFF-R2 |
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Assay List of Neuropeptide FF Receptors
Creative Biolabs can provide a range of assays of neuropeptide FF receptors. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title |
Diet-induced adaptive thermogenesis requires neuropeptide FF receptor-2 signaling |
| Journal |
Nature Communications |
| Published |
2018 |
| Abstract | Excessive caloric intake will lead to fat accumulation, and the organism will produce adaptive thermogenesis to increase energy expenditure to spare weight gain. This effect is frequently observed in humans and rodents. The peripheral signals of this effect have been explored in depth. Brown adipose tissue is the most critical tissue to promote thermogenesis, and studies have revealed that it activates thermogenesis through an uncoupling protein-dependent mechanism. However, much less is known about the central mechanisms of adaptive thermogenesis compared with the advances in peripheral tissues. Previous studies have shown that NPFFR2 can be activated by NPFF, PrRP, and NPVF, and is abundant in the hypothalamus related to the regulation of energy homeostasis. These agonists have been shown to regulate energy metabolism, regulate glucose, and mediate satiety signaling and the thermogenic effects of leptin. Therefore, the researchers defined NPFFR2 as a potential key receptor molecule for diet-induced thermogenesis, and constructed a variety of mouse models to determine the intervention of NPFFR2 signaling on energy balance and thermogenic behavior in complex cross-signaling response pathways. |
| Result |
In order to simplify the multi-receptor response system of NPFFR2, the experimenters constructed a variety of different NPFFR2 mouse models, and systematically examined changes in NPFFR2 signaling during long-term feeding and its impact on body energy balance and parameter changes in thermogenesis regulation. Experimental data suggest that adaptive thermogenesis is dependent on signaling from the NPFFR2 receptor, and that loss of NPFFR2 leads to significant increases in body weight and changes in bone mass. NPFFR2 signaling induces adaptive thermogenesis in activated BAT under conditions of energy surplus without major changes in food intake. Experimental results demonstrate that NPFFR2 signaling can control thermogenic processes and regulation of bone homeostasis through effects on neuronal neuropeptide populations, which can consume large excess energy, disturbance to this pathway leads to the adaptive thermogenesis pathway in BAT not responding to the energy surplus generated by excessive myopia, leading to obesity. Intervention and treatment targeting this pathway may be an effective and potential approach to obesity control.
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Fig.2. NPFFR2 signaling regulates the NPY-PVN-TH pathway. (Sampson, 2018)
Reference
- Zhang, L.; et al. Diet-induced adaptive thermogenesis requires neuropeptide FF receptor-2 signaling. Nature Communications. 2018, 9: 4722.
