Highly potent growth hormone secretagogues: Hybrids of NN703 and ipamorelin

Authors
Hansen, TK Ankersen, M Raun, K Hansen, BS
Citation
Tk. Hansen et al., Highly potent growth hormone secretagogues: Hybrids of NN703 and ipamorelin, BIOORG MED, 11(14), 2001, pp. 1915-1918
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1915 - 1918
Database
ISI
SICI code
0960-894X(20010723)11:14<1915:HPGHSH>2.0.ZU;2-A
Abstract
A series of NN703 analogues with lysine mimetics combined with naphthyl- or biphenylalanine in the core has been prepared and tested in vitro in a rat pituitary cell based assay and subsequently in vivo in pigs in a single do se at 50 nmol/kg. Reintroduction of certain pharmacophores in the C-termina l of NN703. which were originally removed during optimisation for oral bioa vailability, led to unexpectedly potent compounds in vitro as well as in vi vo. (C) 2001 Elsevier Science Ltd. All rights reserved.