Neuropeptide W/neuropeptide B receptors

Overview

The neuropeptide BW receptor 1 (NPBW1, provisional nomenclature [1]) is activated by two 23-amino-acid peptides, neuropeptide W (neuropeptide W-23) and neuropeptide B (neuropeptide B-23) [2,3]. C-terminally extended forms of the peptides (neuropeptide W-30 and neuropeptide B-29) also activate NPBW1 [4]. Unique to both forms of neuropeptide B is the N-terminal bromination of the first tryptophan residue, and it is from this post-translational modification that the nomenclature NPB is derived. These peptides were first identified from bovine hypothalamus and therefore are classed as neuropeptides. Endogenous variants of the peptides without the N-terminal bromination, des-Br-neuropeptide B-23 and des-Br-neuropeptide B-29, were not found to be major components of bovine hypothalamic tissue extracts. The NPBW2 receptor is activated by the short and C-terminal extended forms of neuropeptide W and neuropeptide B [4].

References

  1. Foord SM, Bonner TI, Neubig RR, et al. International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev 2005;57:279-88.
  2. Shimomura Y, Harada M, Goto M, et al. Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8. J Biol Chem 2002;277:35826-32.
  3. Fujii R, Yoshida H, Fukusumi S, et al. Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem 2002;277:34010-6.
  4. Brezillon S, Lannoy V, Franssen JD, et al. Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem 2003;278:776-83.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human
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Assay modes:
Agonist
Inverse agonist
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Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
NPW‐30
EC50:
20 nM
Human
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Assay modes:
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Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
NPW‐30
EC50:
14 nM
Mouse
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Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
NPW‐30
EC50:
61 nM