PancreaticPolypeptide, rat, is an agonist of the NPY receptor with high affinity at NPYR4. Pancreaticpolypeptide (PP) is a 36-amino acid, C-terminally amidated peptide, and a member of the PP-fold peptide family, produced and secreted by the PP cells.
Endogenous high affinity agonist for human NPY Y4 receptor (Ki = 0.056 nM). Believed to play an important role in the function of the gastrointestinal tract.
Potent, selective peptide agonist for the neuropeptide Y Y5 receptor (IC50 values for inhibition of NPY binding to human Y5, Y1, Y2 and Y4 receptors are 0.24, 530, > 500, and 51 nM respectively, Ki at Y5 = 0.1 - 0.15 nM). Stimulates food intake in vivo.
Gastrin-releasing peptide (GRP) is a neuropeptide that stimulates gastrin release. It binds to (Ki = 300 nM) and stimulates amylase secretion in rat pancreatic AR42J cells (EC50 = 0.3 nM). GRP increases proliferation of human liver carcinoma HepG2 and MHCC97H cells but does not affect the proliferation of normal HL-7702 liver cells at a concentration of 1 nM. In vivo, GRP (0.35 nmol/kg/h) increases both pancreatic exocrine secretion and pancreaticpolypeptide (PP) release in rats. It dose-dependently stimulates gastrin, pancreatic amylase, lipase, bilirubin, and acid output and induces gallbladder contraction in humans when administered at doses ranging from 1 to 27 pmol/kg per hour.
Positive allosteric modulator of neuropeptide Y receptor 4 (Y4R). Potentiates Y4R response to pancreaticpolypeptide (PP), neuropeptide Y (NPY) and peptide YY (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