Top ▲
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
« Hide
More detailed introduction
The neuropeptide BW receptor 1 (NPBW1, provisional nomenclature [2]) is activated by two 23-amino-acid peptides, neuropeptide W (neuropeptide W-23 (NPW, Q8N729)) and neuropeptide B (neuropeptide B-23 (NPB, Q8NG41)) [3,12]. C-terminally extended forms of the peptides (neuropeptide W-30 (NPW, Q8N729) and neuropeptide B-29 (NPB, Q8NG41)) also activate NPBW1 [1]. 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 (NPB, Q8NG41) and des-Br-neuropeptide B-29 (NPB, Q8NG41), 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 [1].
NPBW1 receptor
C
Show summary »
More detailed page |
NPBW2 receptor
C
Show summary »
More detailed page |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
Potency measurements were conducted with heterologously-expressed receptors with a range of 0.14-0.57 nM (NPBW1) and 0.98-21 nM (NPBW2). NPBW1-/- mice show changes in social behavior, suggesting that the NPBW1 pathway may have an important role in the emotional responses of social interaction [9]. For a review of the contribution of neuropeptide B/W to social dominance, see Watanabe and Yamamoto, 2015 [14]. It has been reported that neuropeptide W may have a key role in the gating of stressful stimuli when mice are exposed to novel environments [8]. Two antagonists have been discovered and reported to have affinity for NPBW1, ML181 and ML250, the latter exhibiting improved selectivity (~100 fold) for NPBW1 compared to MCH1 receptors [4-5]. Computational insights into the binding of antagonists to this receptor have also been described [10-11].