Table 1

Characterization of neuropeptide Y receptor subtypes

Previous namesPP1Y1-like receptors food intake receptorY5, Y2B, PP2
Agonist order of potencyNPY (0.2 nM) ≥ PYY (0.7 nM) >> PP (>100 nM)NPY (0.7 nM) ≈ PYY (0.7 nM) >> PP (>1000 nM)PP (0.05 nM) > NPY1-b ≈ PYY1-b NPY (0.6 nM) ≥ PYY (1 nM) ≥ PP1-c NPY ≈ PYY > PP1-h
Selective agonists[Leu31,Pro34]NPY1-e NPY13–36 1-f PP
[Pro34]NPY1-e NPY3–36 1-g
[Leu31,Pro34]PYY1-e PYY13–36 1-f
[Pro34]PYY1-e PYY3–36 1-g
Selective antagonistsBIBP 3226
Signal transductionGi/o, adenylyl cyclase inhibitionGi/o, adenylyl cyclase inhibitionGi,o, adenylyl cyclase inhibitionGi/o, adenylyl cyclase inhibitionadenylyl cyclase inhibition
Prototypical cell line, SK-N-MC cellsSMS-KAN cells?food intake stimulation??
 tissue or responseHEL cellsrabbit kidney binding sites
  • 1-a No functional protein is expressed in primates due to a truncation in the sixth transmembrane domain.

  • 1-b While some investigators have detected low nanomolar affinity others have reported values to be greater than 1 μM, particularly in rats.

  • 1-c While rat PP has low affinity at both the rat and human Y5 receptor (230 nM), human PP as higher affinity in both species (4 nM).

  • 1-d Also has high affinity for Y4 receptors (Gehlert et al., 1996b).

  • 1-e Selective relative to Y2.

  • 1-f Selective relative to Y1 and Y5.

  • 1-g Selective relative to Y1.

  • 1-h Limited available data are controversial; the affinity values in parentheses are median values at mammalian receptors as taken from the various studies referenced in the text.