Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.


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:
24 08 2023
Historique:
medline: 25 8 2023
pubmed: 3 8 2023
entrez: 3 8 2023
Statut: ppublish

Résumé

The design and synthesis of a series of 2,7-diazaspiro[4.4]nonane derivatives as potent sigma receptor (SR) ligands, associated with analgesic activity, are the focus of this work. In this study, affinities at S1R and S2R were measured, and molecular modeling studies were performed to investigate the binding pose characteristics. The most promising compounds were subjected to

Identifiants

pubmed: 37535861
doi: 10.1021/acs.jmedchem.3c00959
pmc: PMC10461227
doi:

Substances chimiques

Ligands 0
Receptors, sigma 0
Analgesics 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't Research Support, N.I.H., Extramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

11447-11463

Subventions

Organisme : NEI NIH HHS
ID : R01 EY029409
Pays : United States
Organisme : NINDS NIH HHS
ID : R01 NS124784
Pays : United States

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Auteurs

Maria Dichiara (M)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Francesca Alessandra Ambrosio (FA)

Dipartimento di Medicina Sperimentale e Clinica, Università degli Studi "Magna Græcia" di Catanzaro, Campus "S. Venuta", Viale Europa, 88100 Catanzaro, Italy.

Sang Min Lee (SM)

Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, 1905 W Taylor St, Chicago, Illinois 60612, United States.

M Carmen Ruiz-Cantero (MC)

Departamento de Farmacología e Instituto de Neurociencias, Facultad de Medicina, Universitad de Granada e Instituto de Investigación Biosanitaria de Granada ibs.GRANADA, Avenida de la Investigación, 18016 Granada, Spain.

Jessica Lombino (J)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Adriana Coricello (A)

Dipartimento di Scienze della Salute, Università "Magna Græcia" di Catanzaro, Campus "S. Venuta", 88100 Catanzaro, Italy.

Giosuè Costa (G)

Dipartimento di Scienze della Salute, Università "Magna Græcia" di Catanzaro, Campus "S. Venuta", 88100 Catanzaro, Italy.
Net4Science Academic Spin-Off, Università "Magna Græcia" di Catanzaro, Campus "S. Venuta", 88100 Catanzaro, Italy.

Dhara Shah (D)

Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, 1905 W Taylor St, Chicago, Illinois 60612, United States.

Giuliana Costanzo (G)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Lorella Pasquinucci (L)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Kyung No Son (KN)

Department of Ophthalmology and Visual Sciences, University of Michigan, 1000 Wall Street, Ann Arbor, Michigan 48105, United States.

Giuseppe Cosentino (G)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Rafael González-Cano (R)

Departamento de Farmacología e Instituto de Neurociencias, Facultad de Medicina, Universitad de Granada e Instituto de Investigación Biosanitaria de Granada ibs.GRANADA, Avenida de la Investigación, 18016 Granada, Spain.

Agostino Marrazzo (A)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Vinay Kumar Aakalu (VK)

Department of Ophthalmology and Visual Sciences, University of Michigan, 1000 Wall Street, Ann Arbor, Michigan 48105, United States.

Enrique J Cobos (EJ)

Departamento de Farmacología e Instituto de Neurociencias, Facultad de Medicina, Universitad de Granada e Instituto de Investigación Biosanitaria de Granada ibs.GRANADA, Avenida de la Investigación, 18016 Granada, Spain.

Stefano Alcaro (S)

Dipartimento di Scienze della Salute, Università "Magna Græcia" di Catanzaro, Campus "S. Venuta", 88100 Catanzaro, Italy.
Net4Science Academic Spin-Off, Università "Magna Græcia" di Catanzaro, Campus "S. Venuta", 88100 Catanzaro, Italy.

Emanuele Amata (E)

Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

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Classifications MeSH