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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Hansen TK,Ankersen M,Raun K,Hansen BSdoi
10.1016/s0960-894x(01)00345-6subject
Has Abstractpub_date
2001-07-23 00:00:00pages
1915-8issue
14eissn
0960-894Xissn
1464-3405pii
S0960894X01003456journal_volume
11pub_type
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