PMID: 11314756Apr 21, 2001Paper

Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland

Journal of Endocrinological Investigation
G MuccioliR Deghenghi

Abstract

Ghrelin has been proposed as a natural ligand of the GH secretagogue receptor(s) (GHS-R), which was an orphan receptor activated by synthetic peptidyl (hexarelin) and non-peptidyl (MK-0677) GHS to strongly release GH in animals and humans. Herein we studied: 1) the binding of 125I-labeled human ghrelin to membranes from human hypothalamus and pituitary gland; 2) the ability of human ghrelin (either octanoylated or desoctanoylated), as well as of some GHS and neuropeptides to compete with the radioligand. The saturation binding analysis showed, in both tissues, the existence of a single class of high-affinity binding sites with limited binding capacity. The Bmax (maximal number of binding sites) values of ghrelin receptors in the hypothalamus were significantly greater (p<0.001) than those detected in the pituitary, whereas the Kd (dissociation constant) values in the two tissues were similar. 125I-ghrelin bound to hypothalamic membranes was displaced by ghrelin, hexarelin, MK-0677, various GHS antagonists (EP-80317, [D-Arg1-D-Phe5-D-Trp7,9-Leu11]-substance P) and some natural (cortistatin-14) and synthetic (vapreotide) SRIH-14 agonists. In contrast, no competition was seen in the presence of GHRH-44, SRIH-14 or desoctanoylated ...Continue Reading

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Mar 3, 2001·Journal of Endocrinological Investigation·R DeghenghiG Muccioli

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Citations

Sep 21, 2002·Journal of Endocrinological Investigation·F BroglioR Deghenghi
Apr 14, 2006·Journal of Endocrinological Investigation·S GhelardoniR Zucchi
Jul 29, 2004·Journal of Endocrinological Investigation·P LucidiP De Feo
Sep 1, 2005·Pituitary·Roberta GiordanoEmanuela Arvat
May 27, 2010·Neuroscience Bulletin·Li LiuJun-Xia Xie
Jan 27, 2005·Neuroreport·Yuji TsubotaMasanobu Maeda
Aug 28, 2010·International Journal of Peptides·Manfredi TesauroCarmine Cardillo
Jan 11, 2005·Clinical Endocrinology·E GhigoG Muccioli
May 10, 2012·General and Comparative Endocrinology·Atsushi SudaHironori Ando
Mar 31, 2009·Surgical Oncology·Dimitrios NikolopoulosGregory Kouraklis
Feb 19, 2008·Molecular and Cellular Endocrinology·Fabio BroglioEzio Ghigo
Jul 17, 2007·Trends in Endocrinology and Metabolism : TEM·Fabio BroglioEzio Ghigo
Apr 2, 2014·CNS Neuroscience & Therapeutics·Najat AourzIlse Smolders
Dec 2, 2004·Peptides·Maria Teresa ConconiDomenico Ribatti
Jul 24, 2004·Animal Reproduction Science·T SuginoY Terashima
Jun 19, 2004·Peptides·Mélanie Van CraenenbroeckJason Perret
Aug 23, 2005·General and Comparative Endocrinology·Hiroyuki KaiyaKenji Kangawa
Sep 15, 2011·European Journal of Pharmacology·Giuseppe BiaginiVittorio Locatelli
Jan 13, 2004·Journal of Cardiovascular Pharmacology·Lin ChangChaoshu Tang
Jan 5, 2007·Molecular Biology of the Cell·Nicoletta FilighedduAndrea Graziani
Dec 1, 2007·Proteomics. Clinical Applications·Lucien F HarthoornEric Dransfield
Jun 25, 2014·Hypertension·Yuanjie MaoIchiro Kishimoto
Aug 23, 2006·The British Journal of Nutrition·Mercedes Gil-CamposAngel Gil

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