PeptideYY (PYY) is a 36-amino acid peptide and anorectic gut hormone agonist for the neuropeptide Y receptors Y1, Y2, Y5, and Y6 with EC50 values of 0.7, 0.58, 1, and 0.8 nM, respectively, for supression of forskolin-induced cAMP accumulation. PYY is cleaved in vivo to PYY (3-36) . Release of PYY occurs postprandially in proportion to calorie intake from intestinal enteroendocrine L cells, indicating it may be a satiety signal. In humans, PYY inhibits food intake and gastrointestinal transit in both lean and obese subjects.
PeptideYY (PYY), a novel 36 amino-acid amidated hormone is a component of the complex neuroendocrine control process.PeptideYY (PYY) can mediate its effects through the Neuropeptide Y receptors.
JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptideYY with pIC50s of 7.0 and 7.1 for the human Y2 r
Positive allosteric modulator of neuropeptide Y receptor 4 (Y4R). Potentiates Y4R response to pancreatic polypeptide (PP), neuropeptide Y (NPY) and peptideYY (PYY) (EC50 values are 0.03, 0.4 and 0.5 nM respectively). Shows selectivity for Y4R over Y1R, Y2R and Y5R. Schubert et al (2017) Identification and characterization of the first selective Y4 receptor positive allosteric modulator. J.Med.Chem. 60 7605 PMID:28795803