Highly potent growth hormone secretagogues: hybrids of NN703 and ipamorelin. |
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| Authors: | T K Hansen M Ankersen K Raun B S Hansen |
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| Affiliation: | 1. Department of Cardiology, First Affiliated Hospital of Harbin Medical University, Harbin 150001, China;2. Key Laboratory of Molecular Cardiovascular Science, Ministry of Education, Peking University Health Science Center, Beijing 100191, China;3. Laboratory of Cardiovascular Bioactive Molecule, School of Basic Medical Sciences, Peking University, Beijing 100191, China |
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| 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 dose at 50 nmol/kg. Re-introduction of certain pharmacophores in the C-terminal of NN703, which were originally removed during optimisation for oral bioavailability, led to unexpectedly potent compounds in vitro as well as in vivo. |
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