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Neuropeptide Y GPCR Assays

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Background of Neuropeptide Y Receptor

Neuropeptide Y receptors (NPYRs) represent a large family of G-protein coupled receptors, which comprise at least six subtypes that have been designed as NPY1R to NPY6R. They bind to three different types of ligands with varying degrees of preference and participate in many physiological processes within the human body.

Structure prediction of the Human Neuropeptide Y Receptor Type 2.Fig.1. Structure prediction of the Human Neuropeptide Y Receptor Type 2. (Uniprot ID P49146; obtained from Alphafold)

Distribution and Function of Neuropeptide Y Receptor

The expression of NPYRs can be detected throughout the body. In the central nervous system, NPYRs are distributed in regions of the brain or spinal cord, while in the peripheral nervous system, NPYRs are found mostly in the sympathetic nervous system. NPYRs can regulate nerve and heart activity, control dietary patterns, and participate in mood regulation, and can also be used as a therapeutic target for obesity or depression. Studies have also shown that NPYRs and their agonists can regulate the growth behavior of certain types of cells.

Mechanisms of Neuropeptide Y Receptor

Only five isoforms of NPYRs have been successfully cloned, and NPY3R may exist only as a multimer of others.

Receptor Gene Mechanism Agonists Antagonists
NPY1 receptor NPY1R
  • NPY1R shows a propensity to be activated by peptide YY (PYY) or neuropeptide Y (NPY).
  • NPY1R is normally coupled to Gi/o protein, thereby inhibiting the activity of adenylate cyclase and reducing the level of intracellular cAMP.
  • Neuropeptide Y
  • [Leu31, Pro34]-Neuropeptide Y
  • BIBO 3304 trifluoroacetate
  • BIBP 3226 trifluoroacetate
  • BMS 193885
NPY2 receptor NPY2R
  • NPY2R shows a propensity to be activated by peptide YY (PYY) or neuropeptide Y (NPY).
  • NPY2R is normally coupled to Gi/o protein, thereby inhibiting the activity of adenylate cyclase and reducing the level of intracellular cAMP.
  • Peptide YY
  • Neuropeptide Y
  • BIIE 0246 hydrochloride
  • CYM 9484
  • JNJ 5207787
  • SF11
NPY3 receptor NPY3R
  • NPY3R is more likely to be activated by NPY than other ligands.
  • NPY3R is normally coupled to Gi/o protein, thereby inhibiting the activity of adenylate cyclase and reducing the level of intracellular cAMP.
  • Neuropeptide Y
NPY4 receptor NPY4R
  • NPY4R tends to bind to pancreatic polypeptide (PP).
  • NPY4R is normally coupled to Gi/o protein, thereby inhibiting the activity of adenylate cyclase and reducing the level of intracellular cAMP.
  • Pancreatic polypeptide
NPY5 receptor NPY5R
  • NPY5R can be activated by NPY specifically.
  • NPY5R is normally coupled to Gi/o protein, thereby inhibiting the activity of adenylate cyclase and reducing the level of intracellular cAMP.
  • Neuropeptide Y
  • [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide
  • CGP 71683 hydrochloride
  • L-152,804
  • LU AA33810
NPY6 receptor NPYR6
  • The NPY6R is a non-functional pseudogene in human

Assay List of Neuropeptide Y Receptors

Creative Biolabs can provide a range of assays of neuropeptide Y receptors. You can choose the assay in the list or contact us for more information:

NPY1R NPY2R NPY4R NPY5R
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX689 Magic™ Human NPY1R In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX695 Magic™ Rat NPY1R In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX693 Magic™ Rhesus monkey NPY1R In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-0722-KX162 Magic™ Human NPY1R In Vitro Calcium Assay, HEK293-Ga15 HEK293-Ga15 Calcium Flux Assay
S01YF-1122-KX688 Magic™ Human NPY1R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX694 Magic™ Rat NPY1R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX692 Magic™ Rhesus monkey NPY1R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX690 Magic™ Human NPY1R In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX703 Magic™ Rat NPY2R In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX700 Magic™ Rhesus monkey NPY2R In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-0722-KX163 Magic™ Human NPY2R In Vitro Calcium Assay, HEK293-Ga15 HEK293-Ga15 Calcium Flux Assay
S01YF-1122-KX702 Magic™ Rat NPY2R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX699 Magic™ Rhesus monkey NPY2R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX698 Magic™ Human NPY2R In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX701 Magic™ Rhesus monkey NPY2R In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX704 Magic™ Rat NPY2R In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX711 Magic™ Rat NPY4R In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX709 Magic™ Rhesus monkey NPY4R In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX705 Magic™ Human NPY4R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX710 Magic™ Rat NPY4R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX708 Magic™ Rhesus monkey NPY4R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX707 Magic™ Human NPY4R In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX716 Magic™ Rhesus monkey NPY5R In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX712 Magic™ Human NPY5R In Vitro Calcium Flux Assay CHO-K1-Gqi5 Calcium Flux Assay
S01YF-1122-KX715 Magic™ Rhesus monkey NPY5R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX717 Magic™ Rat NPY5R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX714 Magic™ Human NPY5R In Vitro Radioligand Binding Assay CHO-K1-Gqi5 Radioligand Binding Assay

Published Data

Paper Title

The neuropeptide Y receptor gene repository, phylogeny and comparative expression in allotetraploid common carp

Journal

Scientific Reports

Published

2022

Abstract

The NPY family receptors are specific receptors for the endogenous appetite-stimulating factor neuropeptide Y, which lays the physiological foundation for the transmembrane transport of its related peptides. NPY exists widely in various species and affects the neuroendocrine system, regulating appetite and stress feedback. In order to better understand the evolutionary footprint and functional information of NPYR genes, this study conducted a detailed survey of NPYR genes in 10 representative species, and the NPYR gene abundance, structure, conserved gene sequence, and phylogenetic relationship of allo/autotetraploid and diploid species were analyzed. The researchers speculate that the abundance, distribution, and expression profiles of NPYR among different species can provide us with more comprehensive information on the evolutionary route and functional exploration of NPYR genes, and help us gain a deeper understanding of the evolutionary journey of organisms.

Result

In this study, the researchers selected more than ten representative species expressing NPYR, and explored the evolutionary footprint and tissue distribution of NPYR in different organisms. The focus of the study is the investigation of the NPYR gene in allotetraploid carp. Experiments revealed two isoforms of twelve PNYR genes in allotetraploid carp by multiple alignment, phylogenetic relationship, syntenic analysis, and structural analysis. The analysis results show that the number of NPYR genes in tetraploid species is twice that of diploid species, but the distribution of NPYR genes in autotetraploid and diploid species in the same habitat is not strictly 2:1. suggest that ancient whole-genome duplication events may have been followed by gene loss.

This study clarified the evolutionary fate of the NPYR gene under species-specific whole-genome duplication events in teleosts, especially the evolutionary process of allotetraploid carp after the fourth round of whole-genome duplication. Genome-wide research and expression profile comparison of NPYR may provide new insights and theoretical support for exploring the evolutionary path and specific gene functions of more organisms in the future.

Phylogenetic tree of NPYR in vertebrates.Fig.2. Phylogenetic tree of NPYR in vertebrates. (Zou, 2022)

Reference

  1. Zou, X.; et al. The neuropeptide Y receptor gene repository, phylogeny and comparative expression in allotetraploid common carp. Scientific Reports. 2022, 12: 9449.
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