Identification of specific binding sites for glucagon-like peptide-1 on the posterior lobe of the rat pituitary

Neuroendocrinology
R GökeS P Sheikh

Abstract

Glucagon-like peptide-1 (GLP-1) immunoreactivity has been found in autonomic and neuroendocrine brain regions, whereas only limited data are available regarding the characterization and localization of brain GLP-1 receptors. In the present study, using quantitative in vitro autoradiography, a high density of specific binding sites for GLP-1 was characterized on sections of the posterior pituitary lobe of the rat. Low specific binding of radiolabeled GLP-1 was found in the anterior lobe and no specific binding in the intermediate lobe. To examine the specificity of GLP-1 binding sites, sections of the posterior lobe were incubated with radiolabeled GLP-1 in the presence of various peptides. Radiolabeled [Tyr39]exendin-4, a specific GLP-1 agonist, bound to these receptor sites with the same affinity as GLP-1, while glucagon and vasoactive intestinal peptide (VIP) were unable to displace 125I-GLP-1. Both unlabeled exendin-4 and GLP-1 inhibited this binding with equally high affinity. Using 125I-[Tyr39]exendin-4 as radiolabel, the concentration of biding sites was found to be 7.8 +/- 0.4 fmol/mg tissue. Further analysis of the binding data from experiments with tissue slices revealed the presence of high and low affinity binding si...Continue Reading

Citations

Mar 5, 1999·Molecular Neurobiology·E BlázquezJ A Zueco
Dec 12, 2012·Pharmaceutical Research·Ting ChenLeonid Kagan
May 15, 2002·European Journal of Pharmacology·Juris J MeierMichael A Nauck
Feb 18, 2012·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Wei Gao, William J Jusko
Dec 16, 2010·The Journal of Pharmacology and Experimental Therapeutics·Wei Gao, William J Jusko
Dec 17, 2008·Pharmacological Reviews·Wook Kim, Josephine M Egan
Dec 7, 2013·PloS One·Katharine EakinJonathan P Miller
Jul 30, 2005·Neuromolecular Medicine·Bronwen MartinStuart Maudsley
Mar 23, 2005·Regulatory Peptides·Philip J Larsen, Jens Juul Holst
Feb 19, 2005·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Prasanth K ChelikaniRoger D Reidelberger
Dec 22, 1999·Endocrine Reviews·T J Kieffer, J F Habener
Mar 4, 2014·Physiology·Rémy BurcelinStéphane Dalle
Nov 10, 2005·Journal of Endocrinological Investigation·C M RotellaE Mannucci
Jul 13, 2004·Peptides·Naciye Isbil-Buyukcoskun, Guldal Gulec
Jan 15, 2020·European Thyroid Journal·Muhammed Erkam SencarErman Cakal

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cardiovascular Biology of GLP-1

Glucagon-like peptide 1 (GLP-1) plays a role in glucose metabolism, energy homeostasis, and inflammation suppression. GLP-1 receptor signaling has been shown to impact cardiovascular function. This feed focuses on the role of GLP-1 and GLP-1 receptor agonists on cardiovascular biology.