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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature Y1 receptor Y2 receptor Y4 receptor Y5 receptor y6 receptor
HGNC, UniProt NPY1R, P25929 NPY2R, P49146 NPY4R, P50391 NPY5R, Q15761 NPY6R, Q99463
Rank order of potency neuropeptide Y > peptide YY ≫ pancreatic polypeptide neuropeptide Y > peptide YY ≫ pancreatic polypeptide pancreatic polypeptide > neuropeptide Y = peptide YY neuropeptide Y > peptide YY > pancreatic polypeptide neuropeptide Y = peptide YY > pancreatic polypeptide
Endogenous agonists neuropeptide Y (NPY, P01303), peptide YY (PYY, P10082) PYY‐(3‐36) (PYY, P10082) (pK i 9.2–9.7) [588, 599], neuropeptide Y (NPY, P01303), neuropeptide Y‐(3‐36) (NPY, P01303), peptide YY (PYY, P10082) pancreatic polypeptide (PPY, P01298) (pK i 8.7–10.9) [92, 1152, 1899, 2076] – –
Selective agonists [Leu31,Pro34]NPY (pEC50 7.1) [378], [Leu31,Pro34]PYY (human), [Pro34]NPY, [Pro34]PYY (human) – – [Ala31,Aib32]NPY (pig) (pIC50 8.2) [254] –
Selective antagonists BIBO3304 (pIC50 9.5) [2020], BIBP3226 (pK i 8.1–9.3) [436, 2021] BIIE0246 (pIC50 8.5) [434], JNJ‐5207787 (pIC50 6.9–7.1) [178] – L‐152,804 (pK i 7.6) [901] –
Labelled ligands [3H]BIBP3226 (Antagonist) (pK d 8.7), [125I][Leu31,Pro34]NPY (Agonist) [125I]PYY‐(3‐36) (human) (Agonist) [125I]PP (human) (Agonist) [125I][cPP(1‐7), NPY(19‐23), Ala31, Aib32, Gln34]hPP (Agonist) (pK d 9.2–9.3) [453] – Rat –
Comments Note that Pro34‐containing NPY and PYY can also bind Y4 and Y5 receptors, so strictly speaking are not selective, but are the 'preferred' agonists. – – – The y6 receptor is a pseudogene in humans, but is functional in mouse, rabbit and some other mammals.