Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia.
Analgesia
/ methods
Animals
CHO Cells
Cricetinae
Cricetulus
Dose-Response Relationship, Drug
Humans
Hypotension
/ chemically induced
Hypothermia
/ chemically induced
Male
Neurotensin
/ analogs & derivatives
Pain Measurement
/ drug effects
Protein Binding
/ drug effects
Rats
Rats, Sprague-Dawley
Receptors, Neurotensin
/ agonists
Tyrosine
/ genetics
GPCR ligands
NTS2
Neurotensin peptides
analgesia
receptor selectivity
unnatural amino acids
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
20 11 2019
20 11 2019
Historique:
pubmed:
8
10
2019
medline:
26
9
2020
entrez:
8
10
2019
Statut:
ppublish
Résumé
Neurotensin (NT) exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2. This opioid-independent antinociception represents a potential alternative for pain management. While activation of NTS1 also induces a drop in blood pressure and body temperature, NTS2 appears to be an analgesic target free of these adverse effects. Here, we report modifications of NT at Tyr
Identifiants
pubmed: 31589400
doi: 10.1021/acschemneuro.9b00390
doi:
Substances chimiques
Ntsr2 protein, rat
0
Receptors, Neurotensin
0
Neurotensin
39379-15-2
Tyrosine
42HK56048U
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
4535-4544Subventions
Organisme : Canadian Institute of Health Research
ID : FDN-148413
Pays : International
Organisme : Canadian Institute of Health Research
ID : MOP-123399
Pays : International
Organisme : Canadian Institute of Health Research
ID : MOP-136871
Pays : International