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Table 1 IC50 values (nM) for NTS1 and NTS2

From: Evidence for a role of NTS2 receptors in the modulation of tonic pain sensitivity

Compound

Structure

rNTS1

rNTS2

Neurotensin

pyroGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu-OH

5.0 ± 0.7

9.0 ± 2

NT69L

N-methyl-Arg-Lys-Pro-L-neo-Trp-tert-Leu-Leu-OH

2.2 ± 0.5

3.7 ± 0.4

JMV-431

Boc-Arg-ArgPro-Tyrø(CH2NH)-Ile-Leu-OH

4735 ± 135

19 ± 3.2

Levocabastine

non peptidic

> 10,000

2.7 ± 1.3

  1. Binding potencies of NT and related analogs were determined in competition experiments performed with HEK293 cells expressing either NTS1 or NTS2. Data represent means ± SEM of at least three independent experiments carried out in triplicate.
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Molecular Pain

ISSN: 1744-8069

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