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New active series of growth hormone secretagogues |
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| Authors: | 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 |
| Affiliation: | Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810, Université Montpellier I et II, B.P. 14491, Faculté de Pharmacie, 15 Avenue Charles Flahaut, 34093 Montpellier Cédex 5, France. |
| 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) |
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