New active series of growth hormone secretagogues

被引：70

作者：

Guerlavais, V

Boeglin, D

Mousseaux, D

Oiry, C

Heitz, A

Deghenghi, R

Locatelli, V

Torsello, A

Ghé, C

Catapano, F

Muccioli, G

Galleyrand, JC

Fehrentz, JA

Martinez, J

机构：

[1] Univ Montpellier I, UMR 5810, Lab Aminoacides Peptides & Prot LAPP, Fac Pharm, F-34093 Montpellier 5, France

[2] CBS, UMR 5048, Fac Pharm, F-34093 Montpellier 5, France

[3] Europeptides, Zentaris Grp, F-95108 Argenteuil, France

[4] Univ Milan, Sch Med, Dept Expt Environm Med & Biotechnol, I-20052 Monza, MI, Italy

[5] Univ Turin, Dept Anat Pharmacol & Forens Med, I-10125 Turin, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 07期

关键词：

D O I：

10.1021/jm020985q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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)

引用

页码：1191 / 1203

页数：13

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