New Active Series of Growth Hormone Secretagogues

New growth hormone secretagogue (GHS) analogues were synthesized and evaluated for growth hormone releasing activity. This series derived from EP-51389 is based on a gem-diamino structure. Compounds that exhibited higher in vivo GH-releasing potency than hexarelin in rat (subcutaneous administration...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-03, Vol.46 (7), p.1191-1203
Hauptverfasser:	Guerlavais, Vincent, Boeglin, Damien, Mousseaux, Delphine, Oiry, Catherine, Heitz, Annie, Deghenghi, Romano, Locatelli, Vittorio, Torsello, Antonio, Ghé, Corrado, Catapano, Filomena, Muccioli, Giampiero, Galleyrand, Jean-Claude, Fehrentz, Jean-Alain, Martinez, Jean
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Adult Animals Animals, Newborn Binding, Competitive Biological and medical sciences Cell Line Chemical Sciences Dogs Female Growth Hormone - secretion Hormones. Endocrine system Humans In Vitro Techniques Indoles Injections, Subcutaneous Male Medical sciences Membranes Middle Aged Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Organic chemistry Pharmacology. Drug treatments Pituitary Gland - metabolism Radioligand Assay Rats Rats, Sprague-Dawley Receptors, Cell Surface - metabolism Receptors, G-Protein-Coupled Receptors, Ghrelin Tryptophan - analogs & derivatives
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Zusammenfassung:	New growth hormone secretagogue (GHS) analogues were synthesized and evaluated for growth hormone releasing activity. This series derived from EP-51389 is based on a gem-diamino structure. Compounds that exhibited higher in vivo GH-releasing potency than hexarelin in rat (subcutaneous administration) were then tested per os in beagle dogs and for their binding affinity to human pituitary GHS receptors and to hGHS−R 1a. Compound 7 (JMV 1843, H-Aib-(d)-Trp-(d)-gTrp-formyl) showed high potency in these tests and was selected for clinical studies.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm020985q