Literature DB >> 12240910

EP1572: a novel peptido-mimetic GH secretagogue with potent and selective GH-releasing activity in man.

F Broglio1, F Boutignon, A Benso, C Gottero, F Prodam, E Arvat, C Ghè, F Catapano, A Torsello, V Locatelli, G Muccioli, D Boeglin, V Guerlavais, J A Fehrentz, J Martinez, E Ghigo, R Deghenghi.   

Abstract

EP1572 UMV1843 [Aib-DTrp-DgTrp-CHO]) is a new peptido-mimetic GH secretagogue (GHS) showing binding potency to the GHS-receptor in animal and human tissues similar to that of ghrelin and peptidyl GHS. EP1572 induces marked GH increase after s.c. administration in neonatal rats. Preliminary data in 2 normal young men show that: 1) acute i.v. EP1572 administration (1.0 microg/kg) induces strong and selective increase of GH levels; 2) single oral EP1572 administration strongly and reproducibly increases GH levels even after a dose as low as 0.06 mg/kg. Thus, EP1572 is a new peptido-mimetic GHS with potent and selective GH-releasing activity.

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Year:  2002        PMID: 12240910     DOI: 10.1007/BF03345096

Source DB:  PubMed          Journal:  J Endocrinol Invest        ISSN: 0391-4097            Impact factor:   4.256


  8 in total

Review 1.  Peptidomimetic regulation of growth hormone secretion.

Authors:  R G Smith; L H Van der Ploeg; A D Howard; S D Feighner; K Cheng; G J Hickey; M J Wyvratt; M H Fisher; R P Nargund; A A Patchett
Journal:  Endocr Rev       Date:  1997-10       Impact factor: 19.871

2.  Endocrine activities of ghrelin, a natural growth hormone secretagogue (GHS), in humans: comparison and interactions with hexarelin, a nonnatural peptidyl GHS, and GH-releasing hormone.

Authors:  E Arvat; M Maccario; L Di Vito; F Broglio; A Benso; C Gottero; M Papotti; G Muccioli; C Dieguez; F F Casanueva; R Deghenghi; F Camanni; E Ghigo
Journal:  J Clin Endocrinol Metab       Date:  2001-03       Impact factor: 5.958

Review 3.  Ghrelin: discovery of the natural endogenous ligand for the growth hormone secretagogue receptor.

Authors:  M Kojima; H Hosoda; H Matsuo; K Kangawa
Journal:  Trends Endocrinol Metab       Date:  2001-04       Impact factor: 12.015

Review 4.  Neuroendocrine and peripheral activities of ghrelin: implications in metabolism and obesity.

Authors:  Giampiero Muccioli; Matthias Tschöp; Mauro Papotti; Romano Deghenghi; Mark Heiman; Ezio Ghigo
Journal:  Eur J Pharmacol       Date:  2002-04-12       Impact factor: 4.432

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

Authors:  G Muccioli; M Papotti; V Locatelli; E Ghigo; R Deghenghi
Journal:  J Endocrinol Invest       Date:  2001-03       Impact factor: 4.256

Review 6.  Purification and distribution of ghrelin: the natural endogenous ligand for the growth hormone secretagogue receptor.

Authors:  M Kojima; H Hosoda; K Kangawa
Journal:  Horm Res       Date:  2001

7.  Specific receptors for synthetic GH secretagogues in the human brain and pituitary gland.

Authors:  G Muccioli; C Ghè; M C Ghigo; M Papotti; E Arvat; M F Boghen; M H Nilsson; R Deghenghi; H Ong; E Ghigo
Journal:  J Endocrinol       Date:  1998-04       Impact factor: 4.286

8.  Novel hexarelin analogs stimulate feeding in the rat through a mechanism not involving growth hormone release.

Authors:  A Torsello; M Luoni; F Schweiger; R Grilli; M Guidi; E Bresciani; R Deghenghi; E E Müller; V Locatelli
Journal:  Eur J Pharmacol       Date:  1998-11-06       Impact factor: 4.432

  8 in total
  11 in total

1.  GH secretagogues and hypothalamo-pituitary-adrenal axis.

Authors:  M Boscaro; T Mancini
Journal:  J Endocrinol Invest       Date:  2003-03       Impact factor: 4.256

2.  Ghrelin stimulation of growth hormone-releasing hormone neurons is direct in the arcuate nucleus.

Authors:  Guillaume Osterstock; Pauline Escobar; Violeta Mitutsova; Laurie-Anne Gouty-Colomer; Pierre Fontanaud; François Molino; Jean-Alain Fehrentz; Danielle Carmignac; Jean Martinez; Nathalie C Guerineau; Iain C A F Robinson; Patrice Mollard; Pierre-François Méry
Journal:  PLoS One       Date:  2010-02-11       Impact factor: 3.240

Review 3.  Clinical development of ghrelin axis-derived molecules for cancer cachexia treatment.

Authors:  Sumbul Ali; Ji-an Chen; Jose M Garcia
Journal:  Curr Opin Support Palliat Care       Date:  2013-12       Impact factor: 2.302

4.  Pharmacological characterization of the ghrelin receptor mediating its inhibitory action on inflammatory pain in rats.

Authors:  Valeria Sibilia; Francesca Pagani; Emanuela Mrak; Elisa Dieci; Giovanni Tulipano; Francesco Ferrucci
Journal:  Amino Acids       Date:  2012-03-10       Impact factor: 3.520

5.  Protective but not anticonvulsant effects of ghrelin and JMV-1843 in the pilocarpine model of Status epilepticus.

Authors:  Chiara Lucchi; Giulia Curia; Jonathan Vinet; Fabio Gualtieri; Elena Bresciani; Vittorio Locatelli; Antonio Torsello; Giuseppe Biagini
Journal:  PLoS One       Date:  2013-08-28       Impact factor: 3.240

Review 6.  Pathophysiogenesis of mesial temporal lobe epilepsy: is prevention of damage antiepileptogenic?

Authors:  G Curia; C Lucchi; J Vinet; F Gualtieri; C Marinelli; A Torsello; L Costantino; G Biagini
Journal:  Curr Med Chem       Date:  2014       Impact factor: 4.530

Review 7.  From Belly to Brain: Targeting the Ghrelin Receptor in Appetite and Food Intake Regulation.

Authors:  Ken Howick; Brendan T Griffin; John F Cryan; Harriët Schellekens
Journal:  Int J Mol Sci       Date:  2017-01-27       Impact factor: 5.923

8.  Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants.

Authors:  Michael Lissy; Valentin Demmel; Richard Sachse; Nicola Ammer; Nicky Kelepouris; Vlady Ostrow
Journal:  Clin Pharmacol Drug Dev       Date:  2020-09-22

Review 9.  Targeting the ghrelin receptor: orally active GHS and cortistatin analogs.

Authors:  Romano Deghenghi; Fabio Broglio; Mauro Papotti; Giampiero Muccioli; Ezio Ghigo
Journal:  Endocrine       Date:  2003-10       Impact factor: 3.925

10.  Macimorelin (AEZS-130)-stimulated growth hormone (GH) test: validation of a novel oral stimulation test for the diagnosis of adult GH deficiency.

Authors:  J M Garcia; R Swerdloff; C Wang; M Kyle; M Kipnes; B M K Biller; D Cook; K C J Yuen; V Bonert; A Dobs; M E Molitch; G R Merriam
Journal:  J Clin Endocrinol Metab       Date:  2013-04-04       Impact factor: 5.958

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