[125I]Leu31, Pro34-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: evidence for heterogeneity in pancreatic polypeptide receptors.
Cloned receptors for the PP-fold peptides are subdivided into Y1, Y2, PP1/Y4, Y5 and Y6. NPY and PYY have similar affinity for Y1, Y2, Y5 and Y6 receptors while PP has highest affinity for PP1. Pro34-substituted analogs of NPY and PYY have selectivity for Y1 and Y1-like receptors over Y2 receptors. In the present study, we found the putative Y1-selective radioligand, [125I]Leu31, Pro34-PYY, also binds with high affinity to the rat PP1 receptor in cell lines expressing the receptor. However, in rat brain sections, [125I]Leu31, Pro34-PYY does not appear to bind to the interpeduncular nucleus, a brain region containing a high density of [125I]-bPP binding sites. Therefore, it appears there is additional heterogeneity in receptors recognizing PP.
Gehlert
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DR
Lilly Neuroscience, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. Gehlert_Donald_R@Lilly.com
Schober
D A
DA
Gackenheimer
S L
SL
Beavers
L
L
Gadski
R
R
Lundell
I
I
Larhammar
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D
D000818:Animals; D001921:Brain / Q000378:metabolism; D016466:CHO Cells; D006224:Cricetinae; D005768:Gastrointestinal Hormones / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008024:Ligands; D009478:Neuropeptide Y / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000502:physiology; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000737:chemistry / Q000378:metabolism*; D018026:Receptors, Pancreatic Hormone / Q000737:chemistry / Q000378:metabolism*; D011994:Recombinant Proteins
D005768:Gastrointestinal Hormones; D007457:Iodine Radioisotopes; D008024:Ligands; D009478:Neuropeptide Y; D010446:Peptide Fragments; D017476:Receptors, Neuropeptide Y; D018026:Receptors, Pancreatic Hormone; D011994:Recombinant Proteins; C097212:neuropeptide Y-Y1 receptor; C106655:peptide YY, iodo-Leu(34)-Pro(34)-; C062259:neuropeptide Y, Leu(31)-Pro(34)-