2. Signalwege
  3. GPCR/G Protein
  4. Neuropeptide FF Receptor
  5. NPFFR2 Isoform

NPFFR2

NPFFR2 is a G protein-coupled neuropeptide FF receptor activated by NPFF-related peptides and linked to pain modulation, opioid regulation, and RF-amide peptide signaling[1]. Mechanistically, NPFFR2 signaling regulates nociceptive transmission through CGRP, because NPFFR2 activation increased spinal CGRP and produced hyperalgesia in mouse inflammatory pain models[2]. In cephalic pain models, NPFFR2 knockdown or knockout reduced capsaicin-induced CGRP upregulation in trigeminal ganglion, supporting its use in headache and trigeminovascular pathway research[3]. In metabolic models, loss of NPFFR2 impaired high-fat-diet adaptive thermogenesis, reduced BAT UCP-1 and PGC-1α, and worsened obesity-related phenotypes[4]. Compared with related isoforms, NPFFR2 responds strongly to NPFF peptides, whereas NPFFR1 is activated by RFRPs and regulates reproductive hormone balance[5]. For experimental applications, selective nonpeptidergic NPFF2 agonists derived from aryliminoguanidines showed activity in in vivo pain models[6]. - NPFFR2 models connect nociception, CGRP biology, and trigeminovascular pathway activation in mice[2][3]. - Selective NPFF2 agonists support pharmacological separation from nonselective NPFF1/NPFF2 ligand effects[6].

NPFFR2 Verwandte Produkte (7):

Art. -Nr. Produktname Wirkung Reinheit
  • HY-P1248
    Neuropeptide FF
    		99.35%
    Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, is a NPFF1 and NPFF2 receptors agonist with Ki values of 2.82 nM and 0.21 nM, respectively. Neuropeptide FF induces abstinence syndrome, exerts antiopioid and analgesic effects, releases via calcium-dependent mechanisms from rat spinal cord, regulates memory, autonomic function, and neuroendocrine function, modulates pain and opioid antinociception, reduces food intake, stimulates water intake, alters cardiovascular parameters, and shows differential activity in hypothalamic paraventricular nucleus neurons. Neuropeptide FF is present in mammalian central nervous system and periphery, with NPFF-immunoreactivity increases in rat cerebrospinal fluid during opiate tolerance, and its NPFF gene and NPFF-R2 gene are up-regulated in rat spinal cord and dorsal root ganglia during peripheral inflammation. Neuropeptide FF can be used for the research of opioid tolerance, morphine-induced analgesia, abstinence syndrome, pain, hypertension, nociception, inflammatory pain, and neuropathic pain.
  • HY-P10377
    GUB03385
    		Agonist
    GUB03385 is a long-acting PrRP31 analogue. GUB03385 is a potent dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM). GUB03385 has anti-obesity effect.
  • HY-161405
    NPFF1-R antagonist 1
    		Inhibitor 99.38%
    NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.
  • HY-P11811
    GUB10194
    GUB10194 is a fully potent and selective GPR10 agonist with an EC50 of 15 nM. GUB10194 does not significantly affect body weight or food intake.
  • HY-P10395
    DP50
    		Antagonist
    DP50 is a bifunctional compound that contains an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. DP50 can be used in analgesia-related research.
  • HY-P11810
    GUB08248
    		Agonist
    GUB08248 is a full GPR10 agonist and a partial NPFF2R agonist, with EC50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 inhibits food intake and induces sustained weight loss. GUB08248 can be used in obesity-related research.
  • HY-P10394
    DP32
    		Antagonist
    DP32 is a bifunctional compound that contains an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. DP32 can be used in analgesia-related research.