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NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids

Simeth, Nadja Anita ; Bause, Manuel ; Dobmeier, Michael ; Kling, Ralf C. ; Lachmann, Daniel ; Hübner, Harald ; Einsiedel, Jürgen ; Gmeiner, Peter ; König, Burkhard



Abstract

Stimulation of the NTS2 neurotensin receptor causes antipsychotic effects and leads to a promotion of the l-opioid-independent antinociception, which is important in the modulation of tonic pain sensitivity. We report the synthesis and properties of a small library of peptidic agonists based on the active neurotensin fragment NT(8-13). Two tetrahydrofuran amino acid derivatives were synthesized ...

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