Simeth NA, Bause M, Dobmeier M, Kling R, Lachmann D, Hübner H, Einsiedel J, Gmeiner P, Koenig B (2017)
Publication Status: Published
Publication Type: Journal article, Original article
Publication year: 2017
Publisher: PERGAMON-ELSEVIER SCIENCE LTD
Book Volume: 25
Pages Range: 350-359
Journal Issue: 1
DOI: 10.1016/j.bmc.2016.10.039
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 to replace Tyr(11) in NT (8-13). Additionally, Arg(8), Arg(9), and Ile(12) of the lead peptide were exchanged by Lys, Lys, and Gly, respectively. The new compounds showed substantial NTS2 binding affinity and up to 1000-fold selectivity over NTS1. The highest selectivity (Ki(NTS2): 29 nM, Ki(NTS1): 35,000 nM) was observed for the peptide analog 17(Rtrans). (C) 2016 Elsevier Ltd. All rights reserved.
APA:
Simeth, N.A., Bause, M., Dobmeier, M., Kling, R., Lachmann, D., Hübner, H.,... Koenig, B. (2017). NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids. Bioorganic & Medicinal Chemistry, 25(1), 350-359. https://doi.org/10.1016/j.bmc.2016.10.039
MLA:
Simeth, Nadja A., et al. "NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids." Bioorganic & Medicinal Chemistry 25.1 (2017): 350-359.
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