NPBW1 receptor | Neuropeptide W/neuropeptide B receptors | IUPHAR/BPS Guide to PHARMACOLOGY

NPBW1 receptor

Target id: 303

Nomenclature: NPBW1 receptor

Family: Neuropeptide W/neuropeptide B receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for NPBW1 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 328 8q11.23 NPBWR1 neuropeptides B and W receptor 1
Mouse 7 - 1 (A1-A2) Npbwr1 neuropeptides B/W receptor 1
Rat 7 329 5q12 Npbwr1 neuropeptides B and W receptor 1
Previous and Unofficial Names
GPR7 | G protein-coupled receptor 7 | neuropeptides B/W receptor type 1
Database Links
Specialist databases
GPCRDB npbw1_human (Hs), npbw1_mouse (Mm), npbw1_rat (Rn)
Other databases
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
neuropeptide B-23 {Sp: Human}
neuropeptide B-29 {Sp: Human}
neuropeptide B-23 {Sp: Mouse}
neuropeptide B-29 {Sp: Mouse}
neuropeptide B-23 {Sp: Rat}
neuropeptide B-29 {Sp: Rat}
neuropeptide W-23 {Sp: Human}
neuropeptide W-30 {Sp: Human} , neuropeptide W-30 {Sp: Mouse}
neuropeptide W-23 {Sp: Mouse, Rat}
neuropeptide W-30 {Sp: Rat}
Potency order of endogenous ligands (Human)
neuropeptide B-29 (NPB, Q8NG41) > neuropeptide B-23 (NPB, Q8NG41) > neuropeptide W-23 (NPW, Q8N729) > neuropeptide W-30 (NPW, Q8N729)  [2]

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I][Tyr11]des-Br-NPB-23 Hs Full agonist 10.4 pKd 5
pKd 10.4 [5]
[125I]NPW-23 (human) Rn Full agonist 9.4 pKd 14
pKd 9.4 [14]
neuropeptide W-30 {Sp: Human} Hs Full agonist 10.6 pIC50 13
pIC50 10.6 [13]
neuropeptide W-23 {Sp: Human} Hs Full agonist 10.0 pIC50 13
pIC50 10.0 [13]
des-Br-neuropeptide B-29 {Sp: Human} Hs Full agonist 9.5 pIC50 2,5
pIC50 9.5 [2,5]
neuropeptide B-29 {Sp: Human} Hs Full agonist 9.5 pIC50 5
pIC50 9.5 [5]
des-Br-neuropeptide B-23 {Sp: Human} Hs Full agonist 8.8 pIC50 2,5
pIC50 8.8 [2,5]
View species-specific agonist tables
Agonist Comments
The potency data above is found from several binding assays where the experimental conditions may not be consistent.
Results from functional studies give the rank order of affinity as:
NPB-29 > NPB-23 > NPW-23 > NPW-30 [2].
This order of potency generated from functional assays is generally more accepted than the rank order generated from the binding data, shown below.

Deletion of the first tryptophan residue in both NPB and NPW results in significant reduction in potency suggesting that the N-terminus is involved in receptor binding and signal transduction.
There does not seem to be significant differences in the potency of peptides between humans, rats and mice which may be expected as the peptides share considerable homology with species.
Immunocytochemical localisation studies have reported the presence of these peptides in discrete regions of the central nervous system, particularly within the amygdala and hypothalamus or within the cell bodies of neurones which project to areas expressing the NPBW1 receptor [3-4,14]. In the periphery, NPW-like immunoreactivity has been localised to the renal glomeruli, as well as the endothelium of both the left internal mammary artery and the endocardium. It has yet to be determined whether NPB or NPW circulate in human plasma.

The de-brominated forms of the endogenous ligands neuropeptide B-23 and neuropeptide B-29, des-Br-neuropeptide B-29 and des-Br-neuropeptide-23 were not found to be major components of bovine hypothalamus [5].
Antagonist Comments
No antagonists are currently available for NPBW1.
Allosteric Modulator Comments
It is currently unknown whether there are allosteric regulators for NPBW1.
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Comments:  NPB has been shown to stimulate the Gq/G11 phospholipase C pathway. However, it has not been conclusively determined whether this is through NPBW1 activation or via another receptor.
References:  2,5,13,15
Tissue Distribution
Hippocampus, amygdala, trachea > brain, foetal brain, pituitary, prostate > thalamus, corpus callosum, substantia nigra, foetal spleen, peripheral blood leukocytes, foetal kidney, testis, lung, lung carcinomas, colon, rectum, skin.
Species:  Human
Technique:  RT-PCR.
References:  2
Lateral wings of the pituitary gland.
Species:  Human
Technique:  in situ hybridisation.
References:  11
Adrenal cortex.
Species:  Human
Technique:  RT-PCR.
References:  9
Cerebellum, frontal cortex > pituitary, hypothalamus.
Species:  Human
Technique:  Northern blotting.
References:  11
Discrete localisation in certain areas of the hippocampus, hypothalamus and midbrain.
Hypothalamus: suprachiasmatic nucleus > arcuate nucleus, ventromedial nucleus.
Species:  Mouse
Technique:  in situ hybridisation.
References:  11
Taenia tecta, islands of calleja > olfactory tubercle, primary olfactory cortex > remainder of the cerebral cortex.
Hypothalamus: suprachiasmic nucleus, pararocellular dividion of the paraventricular nucleus > supraoptic, dorsomedial and ventromedial nuclei.
Hippocampus: dentate gyrus and C.A. fields of Ammon's horn.
Medial amygdaloid nucleus.
Species:  Rat
Technique:  in situ hybridisation.
References:  7
Medial amygdaloid nuclei > bed nucleus of the stria terminalis of the thalamus, suprachiasmatic nucleus of the hypothalamus > endopiriform nuclei, medial preoptic area of the hypothalamus and the subfornical organ.
Midbrain: layers of the superior colliculus, periaquaductal grey, and dorsal vagal complex.
Species:  Rat
Technique:  Radioligand binding.
References:  14
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Melanophore aggregation assay.
Species:  Human
Tissue:  Xenopus laevis melanophores transfected with the NPWB1 receptor.
Response measured:  Aggregation of melanosomes.
References:  15
Measurement of cAMP levels in CHO cells transfected with the NPWB1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP production.
References:  2,5,13
Physiological Functions
Modulation of feeding.
Species:  Rat
Tissue:  i.c.v. in vivo study.
References:  1,8,10,12-13
Stimulation of prolactin release.
Species:  Rat
Tissue:  i.c.v. in vivo study.
References:  1,12-13
Stimulation of corticosterone release.
Species:  Rat
Tissue:  i.c.v. in vivo study.
References:  12,16
Inhibition of growth hormone release.
Species:  Rat
Tissue:  i.c.v. in vivo study.
References:  12
Analgesia.
Species:  Rat
Tissue:  In vivo.
References:  15,17-18
Enhanced cortisol secretion.
Species:  Human
Tissue:  Zona fasciculata-reticularis cells of the adrenal gland, in vitro.
References:  9
Physiological Consequences of Altering Gene Expression
Sexual dimorphic effects were observed in NPBW1 knockout mice.
Male knockout mice were hyerphagic and had decreased energy expenditure and locomotor activity. This resulted in the development of adult on-set obesity, independent of the leptin and NPY pathway.
Female knockout mice did not alter in phenotype compared to controls.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  6
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0002118 abnormal lipid homeostasis PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0001392 abnormal locomotor activity PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0005290 decreased oxygen consumption PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0000599 enlarged liver PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0002628 hepatic steatosis PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0001559 hyperglycemia PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0002079 increased circulating insulin level PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0005669 increased circulating leptin level PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0003212 increased susceptibility to age related obesity PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0005658 increased susceptibility to diet-induced obesity PMID: 12925742 
Lepob|Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck,Lepob/Lepob
involves: 129P/Ola * C57BL/6J
MGI:104663  MGI:891989  MP:0001261 obese PMID: 12925742 
a|Ay|Npbwr1tm1Rck Ay/a,Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:87853  MGI:891989  MP:0001261 obese PMID: 12925742 
Npbwr1tm1Rck Npbwr1tm1Rck/Npbwr1tm1Rck
involves: 129P/Ola * C57BL/6J
MGI:891989  MP:0001433 polyphagia PMID: 12925742 
General Comments
Fluorescence in situ hybridisation [11] identified NPBW1 chromosomal localisation to 10q11.2 to 10q21.11 whereas human genome and ensembl characteristics of NPBW1 have identified the chromosomal localisation to 8q11.23.

NPBW1 is predominantly expressed in the central nervous system of mouse, rat and human. However, reports have suggested a peripheral distribution, in particular the renal tubular epithelial cells and the adrenal gland [9]. The distribution in the CNS appears to show good correlation with the function of modulating feeding.

References

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1. Baker JR, Cardinal K, Bober C, Taylor MM, Samson WK. (2003) Neuropeptide W acts in brain to control prolactin, corticosterone, and growth hormone release. Endocrinology., 144: 2816-2821. [PMID:12810535]

2. Brezillon S, Lannoy V, Franssen JD, Le Poul E, Dupriez V, Lucchetti J, Detheux M, Parmentier M. (2003) Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem., 278: 776-783. [PMID:12401809]

3. Dun SL, Brailoiu GC, Mizuo K, Yang J, Chang JK, Dun NJ. (2005) Neuropeptide B immunoreactivity in the central nervous system of the rat. Brain Res., 1045: 157-163. [PMID:15910774]

4. Dun SL, Brailoiu GC, Yang J, Chang JK, Dun NJ. (2003) Neuropeptide W-immunoreactivity in the hypothalamus and pituitary of the rat. Neurosci Lett., 349: 71-74. [PMID:12946555]

5. Fujii R, Yoshida H, Fukusumi S, Habata Y, Hosoya M, Kawamata Y, Yano T, Hinuma S, Kitada C, Asami T, Mori M, Fujisawa Y, Fujino M. (2002) Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem., 277: 34010-34016. [PMID:12118011]

6. Ishii M, Fei H, Friedman JM. (2003) Targeted disruption of GPR7, the endogenous receptor for neuropeptides B and W, leads to metabolic defects and adult-onset obesity. Proc Natl Acad Sci U S A., 100: 10540-10545. [PMID:12925742]

7. Lee DK, Nguyen T, Porter CA, Cheng R, George SR, O'Dowd BF. (1999) Two related G protein-coupled receptors: the distribution of GPR7 in rat brain and the absence of GPR8 in rodents. Brain Res Mol Brain Res., 71: 96-103. [PMID:10407191]

8. Levine AS, Winsky-Sommerer R, Huitron-Resendiz S, Grace MK, De Lecea L. (2005) Injection of neuropeptide W into paraventricular nucleus of hypothalamus increases food intake. Am J Physiol Regul Integr Comp Physiol., 288: R1727-R1732. [PMID:15886360]

9. Mazzocchi G, Rebuffat P, Ziolkowska A, Rossi GP, Malendowicz LK, Nussdorfer GG. (2005) G protein receptors 7 and 8 are expressed in human adrenocortical cells, and their endogenous ligands neuropeptides B and w enhance cortisol secretion by activating adenylate cyclase- and phospholipase C-dependent signaling cascades. J Clin Endocrinol Metab., 90: 3466-3471. [PMID:15797961]

10. Mondal MS, Yamaguchi H, Date Y, Shimbara T, Toshinai K, Shimomura Y, Mori M, Nakazato M. (2003) A role for neuropeptide W in the regulation of feeding behavior. Endocrinology., 144: 4729-4733. [PMID:12959997]

11. O'Dowd BF, Scheideler MA, Nguyen T, Cheng R, Rasmussen JS, Marchese A, Zastawny R, Heng HH, Tsui LC, Shi X et al.. (1995) The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain. Genomics., 28: 84-91. [PMID:7590751]

12. Samson WK, Baker JR, Samson CK, Samson HW, Taylor MM. (2004) Central neuropeptide B administration activates stress hormone secretion and stimulates feeding in male rats. J Neuroendocrinol., 16: 842-849. [PMID:15500544]

13. Shimomura Y, Harada M, Goto M, Sugo T, Matsumoto Y, Abe M, Watanabe T, Asami T, Kitada C, Mori M, Onda H, Fujino M. (2002) Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8. J Biol Chem., 277: 35826-35832. [PMID:12130646]

14. Singh G, Maguire JJ, Kuc RE, Fidock M, Davenport AP. (2004) Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry. Brain Res., 1017: 222-226. [PMID:15261118]

15. Tanaka H, Yoshida T, Miyamoto N, Motoike T, Kurosu H, Shibata K, Yamanaka A, Williams SC, Richardson JA, Tsujino N, Garry MG, Lerner MR, King DS, O'Dowd BF, Sakurai T, Yanagisawa M. (2003) Characterization of a family of endogenous neuropeptide ligands for the G protein-coupled receptors GPR7 and GPR8. Proc Natl Acad Sci U S A., 100: 6251-6256. [PMID:12719537]

16. Taylor MM, Yuill EA, Baker JR, Ferri CC, Ferguson AV, Samson WK. (2005) Actions of neuropeptide W in paraventricular hypothalamus: implications for the control of stress hormone secretion. Am J Physiol Regul Integr Comp Physiol., 288: R270-R275. [PMID:15345475]

17. Yamamoto T, Saito O, Shono K, Tanabe S. (2005) Anti-hyperalgesic effects of intrathecally administered neuropeptide W-23, and neuropeptide B, in tests of inflammatory pain in rats. Brain Res., 1045: 97-106. [PMID:15910767]

18. Zaratin PF, Quattrini A, Previtali SC, Comi G, Hervieu G, Scheideler MA. (2005) Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies. Mol Cell Neurosci., 28: 55-63. [PMID:15607941]

Contributors

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How to cite this page

Anthony P. Davenport, Gurminder Singh.
Neuropeptide W/neuropeptide B receptors: NPBW1 receptor. Last modified on 20/02/2018. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=303.