The present study evaluates the putative differences between NPFF1 and NPFF2 receptor distribution and density throughout the central nervous system between rat and mouse strains by using in vitro quantitative autoradiography. The binding of [125I]YVP ([125I]YVPNLPQRF-NH2) and [125I]EYF ([125I]EYWSLAAPQRF-NH2), used to label NPFF1 and NPFF2 receptors, respectively, was compared between Sprague-Dawley and Wistar rats and between Swiss and C57BL/6-SV129 mice. In contrast to Wistar, Sprague-Dawley brains contained NPFF1 binding sites in the cortical and spinal cord areas, the accumbens nucleus, the anterodorsal thalamic nucleus, the parafascicular thalamic nucleus, the inferior colliculus and the nucleus of the solitary tract. The distribution of NPFF2 binding sites was also different between the two strains of rats. As compared to Swiss, C57BL/6-SV129 mice showed higher basal NPFF2 receptor levels in cortical areas, telencephalon and some other regions. In contrast, they showed lower amounts in thalamic structures, except the reuniens nucleus, and in mesencephalic and rhombencephalic regions. In the cervical spinal cord the levels of NPFF2 receptors were similar. The NPFF1 binding levels were nearly the same in telencephalic structures while distinct in the forebrain. Differences in amount of NPFF receptor subtypes among these strains of rats or mice could lead to differences in NPFF control of opioid nociception.
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http://dx.doi.org/10.1016/j.brainres.2004.04.005 | DOI Listing |
Neuropeptides
December 2024
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Physiology, School of Basic Medical Sciences, State Key Laboratory of Animal Diseases Control, College of Veterinary Medicine, Lanzhou University, 199 Donggang West Road, Lanzhou 730000, PR China. Electronic address:
The neuropeptide FF (NPFF) system regulates various physiological and pharmacological functions, particularly pain modulation. However, the modulatory effect of NPFF system on itch remains unclear. To investigate the modulatory effect and functional mechanism induced by NPFF system on acute itch, we examined the effects of supraspinal administration of NPFF and related peptides on acute itch induced by intradermal (i.
View Article and Find Full Text PDFEur J Med Chem
April 2024
Department of Medicinal Chemistry, College of Pharmacy, The University of Florida, Gainesville, FL, 32610, USA; Department of Pharmaceutics, College of Pharmacy, The University of Florida, Gainesville, FL, 32610, USA; UF Translational Drug Development Core, The University of Florida, Gainesville, FL, 32610, USA.
ACS Chem Neurosci
November 2022
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and Institute of Physiology, School of Basic Medical Sciences, and State Key Laboratory of Veterinary Etiological Biology, College of Veterinary Medicine, Lanzhou University, 199 Donggang West Road, Lanzhou 730000, P. R. China.
Mounting evidence indicates that the neuropeptide FF (NPFF) system is involved in the side effects of opioid usage, including antinociceptive tolerance, hyperalgesia, abuse, constipation, and respiratory depression. Our group recently discovered that the multitarget opioid/NPFF receptor agonist DN-9 exhibits peripheral antinociceptive activity. To improve its metabolic stability, antinociceptive potency, and duration, in this study, we designed and synthesized a novel cyclic disulfide analogue of DN-9, OFP011, and examined its bioactivity through cyclic adenosine monophosphate (cAMP) functional assays and behavioral experiments.
View Article and Find Full Text PDFNeuropharmacology
September 2020
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, And Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China. Electronic address:
Pharmacological evidence indicated a functional interaction between neuropeptide FF (NPFF) and cannabinoid systems, and the cannabinoids combined with the NPFF receptor agonist neuropeptide VF (NPVF) produced antinociception without tolerance. In the present study, VF-13, a chimeric peptide containing the pharmacophores of the endogenous cannabinoid peptide VD-hemopressin(α) (VD-Hpα) and NPVF, was synthesized and pharmacologically evaluated. In vitro, VF-13 significantly upregulated the phosphorylated level of extracellular signal-regulated kinase 1/2 (ERK1/2) in CHO cells stably expressing CB1 receptors and inhibited forskolin-induced cAMP accumulation in HEK293 cells stably expressing NPFF or NPFF receptors.
View Article and Find Full Text PDFBioorg Med Chem
February 2019
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China. Electronic address:
It is well known that opioid analgesics produce side effects including tolerance and constipation. Since neuropeptide FF (NPFF) receptor antagonists reversed opioid-induced hyperalgesia and analgesic tolerance, the present work was performed to synthetize two branched peptidomimetics, EKR and RKE, containing the opioid peptide endomorphin-2 (EM-2) and the NPFF receptor antagonist RF9. Our data obtained from the in vitro cyclic adenosine monophosphate experiment demonstrated that EKR functioned as a mixed mu-, delta-opioid receptors agonist and NPFF receptor antagonist/NPFF receptor partial agonist, whereas RKE acted as a multi-functional peptidomimetic with the mu-opioid agonism and the NPFF antagonism/NPFF partial agonism.
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