Last update 01 Nov 2024

NPFFR1

Last update 01 Nov 2024

Basic Info

Synonyms

G protein-coupled receptor 147, G-protein coupled receptor 147, GPR147

+ [7]

Introduction

Receptor for NPAF (A-18-F-amide) and NPFF (F-8-F-amide) neuropeptides, also known as morphine-modulating peptides. Can also be activated by a variety of naturally occurring or synthetic FMRF-amide like ligands. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.

Drugs associated with NPFFR1

AC-262620

Target

NPFFR1

Mechanism

NPFFR1 inhibitors

Active Org.

ACADIA Pharmaceuticals, Inc.

Originator Org.

Acadia Pharmaceuticals AB

Active Indication

Smoking Cessation

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

RF-313

Target

NPFFR1

Mechanism

NPFFR1 inhibitors

Active Org.

University of Strasbourg

Originator Org.

University of Strasbourg

Active Indication

Hyperalgesia

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

RF3286

Target

NPFFR1

Mechanism

NPFFR1 inhibitors

Active Org.

University of Strasbourg

Originator Org.

University of Strasbourg

Active Indication

Hyperalgesia

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with NPFFR1

100 Translational Medicine associated with NPFFR1

0 Patents (Medical) associated with NPFFR1

131

Literatures (Medical) associated with NPFFR1

08 Aug 2024·The World Journal of Biological Psychiatry

Late maternal separation provides resilience to chronic variable stress-induced anxiety- and depressive-like behaviours in male but not female mice

Article

Author: Dongre, Shweta ; Srivastava, Raj Kamal ; Singh, Padmasana ; Ojha, Rajesh Kumar

Maternal separation can have long-lasting effects on an individual's susceptibility to stress later in life. Maternal separation during the postnatal period is a commonly used paradigm in rodents to investigate the effects of early life stress on neurobehavioural changes and stress responsiveness. However, maternal separation during stress hyporesponsive and responsive periods of postnatal development may differ in its effects on stress resilience. Therefore, we hypothesised that late maternal separation (LMS) from postnatal day 10 to 21 in mice may have different effect on resilience than early maternal separation during the first week of postnatal life. Our results suggested that male LMS mice are more resilient to chronic variable stress (CVS)-induced anxiety and depressive-like behaviour as confirmed by the open field, light-dark field, elevated plus maze, sucrose preference and tail suspension tests. In contrast, female LMS mice were equally resilient as non-LMS female mice. We found increased expression of NPY, NPY1R, NPY2R, NPFFR1, and NPFFR2 in the hypothalamus of male LMS mice whereas the opposite effect was observed in the hippocampus. LMS in male and female mice did not affect circulating corticosterone levels in response to psychological or physiological stressors. Thus, LMS renders male mice resilient to CVS-induced neurobehavioural disorders in adulthood.

01 Jul 2024·3 Biotech

Functional transcriptome analysis revealed major changes in pathways affecting systems biology of Tharparkar cattle under seasonal heat stress

Article

Author: Gowane, Gopal R ; Dutta, Gaurav ; Singh, Ayushi ; Ludri, Ashutosh ; Verma, Archana ; Alex, Rani

Heat stress significantly disturbs the production, reproduction, and systems biology of dairy cattle. A complex interaction among biological systems helps to combat and overcome heat stress. Indicine cattle breed Tharparkar has been well known for its thermal adaptability. Therefore, present investigation considered RNA-seq technology to explore the functional transcriptomics of Tharparkar cattle with the help of samples collected in spring and summer season. Among differentially expressed genes, about 3280 genes were highly dysregulated, in which 1207 gene were upregulated and 2073 genes were downregulated (|log2fold change|≥ 1 and p ≤ 0.05). Upregulated genes were related to insulin activation, interferons, and potassium ion transport. In contrast, downregulated genes were related to RNA processing, translation, and ubiquitination. Functional annotation revealed that the pathways associated with nervous system (NPFFR1, ROBO3) and metal ion transport (KCNG2, ATP1A2) were highly activated while mRNA processing and translation (EIF4A, EIF4B) and protein processing pathway (VPS4B, PEX13) were highly downregulated. Protein-protein interactions identified hub genes such as ATP13A3, IFNGR2, UBXN7, EIF4A2, SLC12A8 found to play an important role in immune, ubiquitination, translation and transport function. Co-expression network includes LYZ, PNRC1, SQSTM1, EIF4AB and DDX17 genes which are involved in lysosomal activity, tumor inhibition, ubiquitination, and translation initiation. Chemokine signaling pathway associated with immune response was highly upregulated in cluster analysis. The findings of this study provide insights into transcriptome expression and regulation which may better explain complex thermal resilience mechanism of Tharparkar cattle in heat stress under natural conditions.Supplementary InformationThe online version contains supplementary material available at 10.1007/s13205-024-04018-2.

09 May 2024·Journal of Medicinal Chemistry

Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects

Article

Author: Schneider, Séverine ; Ces, Aurelia ; Ballet, Steven ; Gonzalez, Simon ; Daubeuf, François ; Lecat, Sandra ; Kremer, Mélanie ; Elhabazi, Khadija ; Herby, Claire ; De Neve, Jolien ; Bihel, Frédéric ; Fellmann-Clauss, Rosine ; Petit-Demouliere, Nathalie ; Simonin, Frédéric ; Utard, Valérie ; Martin, Charlotte

The design of bifunctional compounds is a promising approach toward the development of strong analgesics with reduced side effects. We here report the optimization of the previously published lead peptide KGFF09, which contains opioid receptor agonist and neuropeptide FF receptor antagonist pharmacophores and is shown to induce potent antinociception and reduced side effects. We evaluated the novel hybrid peptides for their in vitro activity at MOP, NPFFR1, and NPFFR2 and selected four of them (DP08/14/32/50) for assessment of their acute antinociceptive activity in mice. We further selected DP32 and DP50 and observed that their antinociceptive activity is mostly peripherally mediated; they produced no respiratory depression, no hyperalgesia, significantly less tolerance, and strongly attenuated withdrawal syndrome, as compared to morphine and the recently FDA-approved TRV130. Overall, these data suggest that MOP agonist/NPFF receptor antagonist hybrids might represent an interesting strategy to develop novel analgesics with reduced side effects.

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NPFFR1

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