| Abstract
| - The neurotensin C-terminal hexapeptide, NT(8−13), which has been found to adopt a β-strand-like conformation while bound to the NT1 receptor, was modified by the introduction ofconformational constraints. Synthesis of the four stereoisomeric 4.4-spirolactams 1−4 andsubsequent NT1 receptor binding studies showed that the restriction of ψ(Pro10) to approximately 130° leads to a more than 1000-fold increase of binding affinity for 1 (Ki = 12 nM)when compared to the more flexible analogue [NMeTyr11]NT(8−13).
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