The neuropeptide Y Y1 receptor selective radioligand, [125I][Leu31,Pro34]peptide YY, is also a high affinity radioligand for human pancreatic polypeptide 1 receptors.
A number of receptors for the pancreatic polypeptide-fold peptides are proposed based on findings from pharmacology and molecular biology studies. Neuropeptide Y and peptide YY have similar affinity for neuropeptide Y Y1 and neuropeptide Y Y2 while pancreatic polypeptide has highest affinity for pancreatic polypeptide 1. Pro34-substituted analogs of neuropeptide Y and peptide YY have selectivity for neuropeptide Y Y1 over neuropeptide Y Y2 receptors. In the present study, we found that one such 'neuropeptide Y Y1-selective' radioligand, [125I][Leu31,Pro34]peptide YY, also binds with high affinity to the pancreatic polypeptide 1 receptor. Therefore, caution needs to be exercised when using Pro34-analogs to define the neuropeptide Y Y1 receptor in vivo and using tissue preparations.
Gehlert
D R
DR
Central Nervous System and Endocrine Research, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. Gehlert_Donald_R@Lilly.com
Gackenheimer
S L
SL
Schober
D A
DA
Beavers
L
L
Gadski
R
R
Burnett
J P
JP
Mayne
N
N
Lundell
I
I
Larhammar
D
D
D002460:Cell Line; D006801:Humans; D007457:Iodine Radioisotopes; D009478:Neuropeptide Y / Q000031:analogs & derivatives* / Q000378:metabolism; D011869:Radioligand Assay; D011964:Receptors, Gastrointestinal Hormone / Q000378:metabolism*; D017476:Receptors, Neuropeptide Y / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
D007457:Iodine Radioisotopes; D009478:Neuropeptide Y; D011964:Receptors, Gastrointestinal Hormone; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins; C097212:neuropeptide Y-Y1 receptor; C029438:receptors, pancreatic polypeptide-specific; C062259:neuropeptide Y, Leu(31)-Pro(34)-