Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic.

Analgesics / chemical synthesis Animals Drug Design Male Molecular Structure Neurotensin / analogs & derivatives Pain / drug therapy Peptide Fragments / chemical synthesis Peptides, Cyclic / chemical synthesis Rats, Sprague-Dawley Receptors, Neurotensin / metabolism Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
25 02 2021
Historique:
pubmed: 5 2 2021
medline: 5 5 2021
entrez: 4 2 2021
Statut: ppublish

Résumé

Neurotensin (NT) receptor type 2 (NTS2) represents an attractive target for the development of new NT-based analgesics. Here, we report the synthesis and functional

Identifiants

DOI: 10.1021/acs.jmedchem.0c01726 PMID: 33538583
pubmed: 33538583
doi: 10.1021/acs.jmedchem.0c01726
doi:

Substances chimiques

Analgesics 0
Ntsr2 protein, rat 0
Peptide Fragments 0
Peptides, Cyclic 0
Receptors, Neurotensin 0
Neurotensin 39379-15-2

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

2110-2124

Subventions

Organisme : CIHR
ID : FDN-148413
Pays : Canada

Auteurs

Magali Chartier (M)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.

Michael Desgagné (M)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.

Marc Sousbie (M)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.

Jérôme Côté (J)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.

Jean-Michel Longpré (JM)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.

Eric Marsault (E)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.
ORCID: 0000-0002-5305-8762

Philippe Sarret (P)

Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Quebec J1H 5N4, Canada.
ORCID: 0000-0002-7627-701X

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Analgésiques › Design, Structural Optimization, and...
questionsmedicales.fr › Eucaryotes › Animaux › Design, Structural Optimization, and...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Design, Structural Optimization, and...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Design, Structural Optimization, and...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Neuropeptides › Neurotensine › Design, Structural Optimization, and...
questionsmedicales.fr › Phénomènes physiologiques de l'appareil locomoteur et du système nerveux › Phénomènes physiologiques du système nerveux › Sensation › Douleur › Design, Structural Optimization, and...
questionsmedicales.fr › Acides aminés, peptides et protéines › Peptides › Fragments peptidiques › Design, Structural Optimization, and...
questionsmedicales.fr › Acides aminés, peptides et protéines › Peptides › Peptides cycliques › Design, Structural Optimization, and...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Design, Structural Optimization, and...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur aux neuropeptides › Récepteur neurotensine › Design, Structural Optimization, and...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Design, Structural Optimization, and...