Request Demo

Last update 08 May 2025

NPFFR1

Last update 08 May 2025

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

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

DT095597

Target

NPFFR1

Mechanism

NPFFR1 inhibitors

Active Org.

Domain Therapeutics SA

Originator Org.

Domain Therapeutics SA

Active Indication

Chronic Pain [+1]

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

01 Mar 2025·Reproduction in Domestic Animals

New Insights in Bovine Follicular Cysts

Article

Author: Cicirelli, Vincenzo ; Rizzo, Annalisa ; Martino, Nicola Antonio ; Frattina, Lorenza ; Burgio, Matteo ; Carbonari, Alice ; Dell'Aquila, Maria Elena

ABSTRACTThe aim of the present study was to understand the involved factors in follicular cysts in dairy cows. The study consisted of an in vivo and in vitro approach. The in vivo part, hormonal evaluation (Kisspeptin‐10 [Kp‐10], Gonadotropin inhibiting hormone [GnIH], Luteinizing hormone [LH], Oestrogens [E2] and cortisol) was performed in sera of both healthy (H) and cows with follicular cysts (FC). The in vitro part was concentrated on estimating the distribution of GPR54 (Kp‐10 receptor) and GPR147 (GnIH receptor) on cystic and preovulatory follicles. Serum concentrations of Kp‐10, GnIH, LH, E2 and cortisol were significantly higher in Group FC compared with Group H. Gene expression analysis showed a reduction in GPR54 mRNA levels in FC compared to preovulatory follicles, while no expression of the GPR147 receptor was detected. The lower presence of GPR54 in FC compared to the preovulatory follicle can be determined by a down‐receptor regulation induced by elevated serum concentrations of Kp‐10 in cows with ovarian FC. Endocrine imbalances of the hypothalamic–pituitary–ovarian axis, characterising FC, may reflect altered patterns of Kp‐10 and GnIH secretion.

03 Feb 2025·Angewandte Chemie International Edition

Hederagenin is a Highly Selective Antagonist of the Neuropeptide FF Receptor 1 that Reveals Mechanisms for Subtype Selectivity

Article

Author: Tydings, Claiborne ; Meiler, Jens ; Urban, Nicole ; Beck‐Sickinger, Annette G. ; Liessmann, Fabian ; Stichel, Jan ; Schermeng, Tina ; Schaefer, Michael ; Lentschat, Hannah

AbstractRF‐amide peptide receptors including the neuropeptide FF receptor 1 (NPFFR1) are G protein‐coupled receptors (GPCRs) that modulate diverse physiological functions. High conservation of endogenous ligands and receptors makes the identification of selective ligands challenging. Previously identified antagonists mimic the C‐terminus of peptide ligands and lack selectivity towards the closely related neuropeptide FF receptor 2 (NPFFR2) or the neuropeptide Y1 receptor (Y1R). In a high‐throughput screening, we identified the pentacyclic triterpenoid hederagenin (1) as a novel selective antagonist for the NPFFR1. Hederagenin (1) is a natural product isolated from Hedera helix (ivy). We characterized its mode of activity using in vitro and in silico methods, revealing an overlapping binding site of the small molecule with the orthosteric peptide agonists. Despite the high similarity of the orthosteric binding pockets of NPFFR1 and NPFFR2, hederagenin (1) shows strong subtype selectivity, particularly caused by slight differences in the shape of the binding pockets and the rigidity of the small molecule. Several residues inhibiting the activity of hederagenin (1) at the NPFFR2 were identified. As NPFFR1 antagonists are discussed as potential candidates for the treatment of chronic pain, these insights into the structural determinants governing subtype specificity will facilitate the development of next‐generation analgesics with improved safety and efficacy.

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.

Analysis

Perform a panoramic analysis of this field.

view full example data

Hiro LS Researcher

The AI Search Engine Built to Accelerate Biopharma Decisions

Search across billion-scale life sciences data to uncover signals, validate evidence, and act with confidence.

Ask any biopharma research question→

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, Patsnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Discover Synapse Data Servers

Synapse data is now integrated into the PatSnap LS Model Context Protocol (MCP) service. Customize your LLM agent now using our MCP server!

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

NPFFR1

Basic Info

Related

Analysis