Data Set Describing The In Vitro Biological Activity Of Jmv2009, A Novel Silylated Neurotensin(8-13) Analog

Neurotensin (NT) is a tridecapeptide displaying interesting antinociceptive properties through its action on its receptors, NTS1 and NTS2. Neurotensin-like compounds have been shown to exert better antinociceptive properties than morphine at equimolar doses. In this article, we characterized the molecular effects of a novel neurotensin (8-13) (NT(8-13)) analog containing an unnatural amino acid. This compound, named JMV2009, displays a Silaproline in position 10 in re placement of a proline in the native NT(8-13). We first exam-ined the binding affinities of this novel NT(8-13) derivative at both NTS1 and NTS2 receptor sites by performing com-petitive displacement of iodinated NT on purified cell mem-branes. Then, we evaluated the ability of JMV2009 to acti-vate NTS1-related G proteins as well as to promote the re-cruitment of beta-arrestins 1 and 2 by using BRET-based cel-lular assays in live cells. We next assessed its ability to in-duce p42/p44 MAPK phosphorylation and NT receptors inter-nalization using western blot and cell-surface ELISA, respec-tively. Finally, we determined the in vitro plasma stability of this NT derivative. This article is associated with the origi-nal article "Pain relief devoid of opioid side effects following central action of a silylated neurotensin analog" published in European Journal of Pharmacology [1] . The reader is directed to the associated article for results interpretation, comments, and discussion. (c) 2020 The Author(s). Published by Elsevier Inc. This is an open access article under the CC BY license. (http://creativecommons.org/licenses/by/4.0/ )