Neuropeptide Y receptors

Overview

Neuropeptide Y (NPY) receptors are activated by the endogenous peptides neuropeptide Y, neuropeptide Y-(3-36), peptide YY, PYY-(3-36) and pancreatic polypeptide (PP). The receptor originally identified as the Y3 receptor has... [read more] been identified as the CXCR4 chemokine recepter (originally named LESTR, [1]). 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 [2]. 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 [3]. 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).

References

1. Loetscher M, Geiser T, O'Reilly T, et al. Cloning of a human seven-transmembrane domain receptor, LESTR, that is highly expressed in leukocytes. J Biol Chem 1994;269:232-7.
2. Gregor P, Millham ML, Feng Y, et al. Cloning and characterization of a novel receptor to pancreatic polypeptide, a member of the neuropeptide Y receptor family. FEBS Lett 1996;381:58-62.
3. Eriksson H, Berglund MM, Holmberg SK, et al. The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. Regul Pept 1998;75-76:29-37.

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