[摘要]：The synthesis, biol. evaluation, and conformational anal. of 4-amino-indolo[2,3-c]azepin-3-one (Aia)-contg. SRIF mimetics, i.e. I譚FA, are reported. Different subtype selectivities are obsd. depending on the N- and C-terminal substituents of the D-Aia-Lys dipeptide mimetic. An sst5-selective analog with subnanomolar binding affinity was obtained that is the most potent agonist reported to date. A nonselective mimetic with high potency was also identified. This study allows a better definition of the bioactive conformation of the essential D-Trp side chain in the somatostatin pharmacophore.
