Pharmacological characterization of neuropeptide Y-(2-36) binding to neuropeptide Y Y1 and Y2 receptors. 1996

D A Schober, and S L Gackenheimer, and D R Gehlert
CNS Research, Lilly Research Laboratories, Eli Lilly and Co., Lilly Corporate Center, Indianapolis, IN 46285, USA.

Neuropeptide Y-(2-36) has been reported by several research groups to be a more potent orexigenic agent than intact neuropeptide Y. Therefore, it has been proposed that a novel 'Y1 variant' may modulate ingestive behavior. To define the receptor subtype involved in neuropeptide Y-stimulated feeding behavior, we evaluated the binding properties of neuropeptide Y-(2-36) and [125I]neuropeptide Y-(2-36) in established neuropeptide Y1 and Y2 containing cell lines and tissues. Neuropeptide Y-(2-36) displaced [125I]peptide YY binding to SK-N-MC cells (neuropeptide Y Y1 receptors) with a Ki of 3.69 nmol and SK-N-BE(2) cells (neuropeptide Y Y2 receptors) with a Ki of 3.08 nmol. Neuropeptide Y-(2-36) also displaced [125I]peptide YY binding to rat cerebral cortex, hippocampus and olfactory bulb with similar affinities. To examine the brain distribution of [125I]peptide YY, [125I]neuropeptide Y and [125I]neuropeptide Y-(2-36), adjacent sections were labeled and the binding sites detected by autoradiography. A similar distribution of binding was observed for each radioligand in all regions examined. Therefore, neuropeptide Y-(2-36) binds non-selectively to neuropeptide Y Y1 and neuropeptide Y Y2 receptors, but with lower affinity than neuropeptide Y and peptide YY. The increased potency and selectivity seen with neuropeptide Y-(2-36) in feeding studies cannot be explained on the basis of a unique in vitro pharmacology.

UI MeSH Term Description Entries
D007457 Iodine Radioisotopes Unstable isotopes of iodine that decay or disintegrate emitting radiation. I atoms with atomic weights 117-139, except I 127, are radioactive iodine isotopes. Radioisotopes, Iodine
D008297 Male Males
D009478 Neuropeptide Y A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones. Neuropeptide Y-Like Immunoreactive Peptide,Neuropeptide Tyrosine,Neuropeptide Y Like Immunoreactive Peptide,Tyrosine, Neuropeptide
D010446 Peptide Fragments Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques. Peptide Fragment,Fragment, Peptide,Fragments, Peptide
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001345 Autoradiography The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed) Radioautography
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats

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