Y1 | Y2 | Y4 | Y5 | Y61-a | |
---|---|---|---|---|---|
Previous names | — | — | PP1 | Y1-like receptors food intake receptor | Y5, Y2B, PP2 |
Agonist order of potency | NPY (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 antagonists | BIBP 3226 | — | — | — | — |
GR231181-d | |||||
Signal transduction | Gi/o, adenylyl cyclase inhibition | Gi/o, adenylyl cyclase inhibition | Gi,o, adenylyl cyclase inhibition | Gi/o, adenylyl cyclase inhibition | adenylyl cyclase inhibition |
Prototypical cell line, | SK-N-MC cells | SMS-KAN cells | ? | food intake stimulation? | ? |
tissue or response | HEL cells | rabbit 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.