Neuropeptide Y receptors C
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).
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Neuropeptide Y (NPY) receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Neuropeptide Y Receptors [17]) are activated by the endogenous peptides neuropeptide Y (NPY, P01303), neuropeptide Y-(3-36), peptide YY (PYY, P10082), PYY-(3-36) and pancreatic polypeptide (PPY, P01298) (PP). The receptor originally identified as the Y3 receptor has been identified as the CXCR4 chemokine recepter (originally named LESTR, [15]). The y6 receptor is a functional gene product in mouse, absent in rat, but contains a frame-shift mutation in primates producing a truncated non-functional gene [12]. Three-dimensional structures have been determined for subtype active receptors Y1, Y2 and Y4 [14,22] and inactive antagonist bound Y1 and Y2 receptors [21,27]. Many of the agonists exhibit differing degrees of selectivity dependent on the species examined. For example, the potency of PP is greater at the rat Y4 receptor than at the human receptor [8]. In addition, many agonists lack selectivity for individual subtypes, but can exhibit comparable potency against pairs of NPY receptor subtypes, or have not been examined for activity at all subtypes. [125I]-PYY or [125I]-NPY can be used to label Y1, Y2, Y5 and y6 subtypes non-selectively, while [125I][cPP(1-7), NPY(19-23), Ala31, Aib32, Gln34]hPP may be used to label Y5 receptors preferentially (note that cPP denotes chicken peptide sequence and hPP is the human sequence).
Receptors
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Y1 receptor
C
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Y2 receptor
C
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Y4 receptor
C
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Y5 receptor
C
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y6 receptor
C
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Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
The Y1 agonists indicated are selective relative to Y2 receptors. BIBP3226 is selective relative to Y2, Y4 and Y5 receptors [10]. NPY-(13-36) is Y2 selective relative to Y1 and Y5 receptors. PYY-(3-36) is Y2 selective relative to Y1 receptors. Note that Pro34-containing NPY and PYY can also bind Y4 and Y5, thus they are selective only relative to Y2. The y6 receptor is a pseudogene in humans, but is functional in mouse, rabbit and some other mammals.