Disease relevance of NPFFR1

• RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia [1].

High impact information on NPFFR1

• The NPFF receptor appears to be coupled to a G-protein, but details of the second messenger systems have not been clarified yet [2].
• First we showed that 3T3-L1 adipocytes express both NPFF-R1 and NPFF-R2 transcripts, and that NPAF binds adipocyte membranes with a nanomolar affinity as assessed by surface plasmon resonance technology [3].
• Two G protein-coupled receptors (NPFF1 and NPFF2 receptors) have been identified for neuropeptide FF [4].
• The affinity and functional activity of several related RFamide peptides were determined at the human neuropeptide FF receptor subtype 2 (hNPFF2) and the human prolactin-releasing peptide (hPrRP) receptors [5].
• Our study indicated a generally relatively low level of discrimination for RFamide peptides at the NPFF receptor, whereas the hPrRP receptor clearly preferred PrRP or very closely related peptides [5].

Anatomical context of NPFFR1

• Chinese hamster ovary (CHO) cell membranes expressing NPFFR bound [(125)I]-EYF with a K(d) of 0.06 nM [6].
• 4. Membranes from NPFFR expressing CHO cells bound GTP gamma[(35)S] in the presence of SQA-NPFF [6].
• 6. RT -- PCR analysis of human tissues mRNA revealed that expression of NPFFR was mainly detected in placenta, thymus and at lower levels in pituitary gland, spleen and testis [6].
• NPFF and NPFF receptor mRNAs are highly expressed and localized in the superficial layers of the dorsal cord, the two genes are also in dorsal root ganglia though at much lower level [7].

Associations of NPFFR1 with chemical compounds

• The usefulness of BIBP3226 as an antagonist tool on the NPFF receptor is thus limited [8].
• 5. SQA-NPFF inhibited forskolin induced cyclic AMP accumulation in recombinant CHO cells in a dose dependent manner [6].

Other interactions of NPFFR1

• The FP HTS system provides a specific, sensitive and reproducible methodology for studying and screening NPFF receptor ligands [9].

Analytical, diagnostic and therapeutic context of NPFFR1

• The seemingly promiscuous binding of the RFamide peptides to the NPFF receptor was further confirmed by receptor autoradiography [5].
• In contrast, two high anti-peptide ELISA titer but celTRF-negative antibodies failed to recognize the NPFF1 receptor in IHC [10].

References