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.(1)

Guerlavais, V., Boeglin, D., Mousseaux, D., Oiry, C., Heitz, A., Deghenghi, R., et al. (2003). New active series of growth hormone secretagogues. JOURNAL OF MEDICINAL CHEMISTRY, 46(7), 1191-1203 [10.1021/jm020985q].

New active series of growth hormone secretagogues

LOCATELLI, VITTORIO;TORSELLO, ANTONIO BIAGIO;
2003

Abstract

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.(1)
Articolo in rivista - Articolo scientifico
Administration, Oral; Animals; Pituitary Gland; Membranes; Humans; Radioligand Assay; Receptors, Cell Surface; Receptors, G-Protein-Coupled; Rats; Receptors, Ghrelin; Animals, Newborn; Rats, Sprague-Dawley; Adult; Binding, Competitive; Dogs; Injections, Subcutaneous; Middle Aged; Oligopeptides; Cell Line; Female; Male; Growth Hormone
English
27-mar-2003
46
7
1191
1203
none
Guerlavais, V., Boeglin, D., Mousseaux, D., Oiry, C., Heitz, A., Deghenghi, R., et al. (2003). New active series of growth hormone secretagogues. JOURNAL OF MEDICINAL CHEMISTRY, 46(7), 1191-1203 [10.1021/jm020985q].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/37156
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