Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.

Allosteric Regulation Amides / chemistry Animals Biological Availability CHO Cells Carbamates / chemistry Cricetulus Dogs Excitatory Amino Acid Agents / chemistry Humans Ligands Rats Receptor, Metabotropic Glutamate 5 / drug effects Structure-Activity Relationship Sulfonamides / chemistry Urea / chemistry

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:
14 02 2019
Historique:
pubmed: 10 1 2019
medline: 4 3 2020
entrez: 10 1 2019
Statut: ppublish

Résumé

Negative allosteric modulators (NAMs) of the metabotropic glutamate receptor 5 (mGlu

Identifiants

DOI: 10.1021/acs.jmedchem.8b01226 PMID: 30624919
pubmed: 30624919
doi: 10.1021/acs.jmedchem.8b01226
doi:

Substances chimiques

Amides 0
Carbamates 0
Excitatory Amino Acid Agents 0
GRM5 protein, human 0
Ligands 0
Receptor, Metabotropic Glutamate 5 0
Sulfonamides 0
Urea 8W8T17847W

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1246-1273

Auteurs

Davide Graziani (D)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.
ORCID: 0000-0003-1826-5392

Silvia Caligari (S)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Elisa Callegari (E)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Carlo De Toma (C)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Matteo Longhi (M)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Fabio Frigerio (F)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Roberto Dilernia (R)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Sergio Menegon (S)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Luca Pinzi (L)

Department of Life Sciences , University of Modena and Reggio Emilia , Via Campi 103 , 41125 Modena , Italy.

Lorenza Pirona (L)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Valerio Tazzari (V)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Anna Elisa Valsecchi (AE)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

Giulio Vistoli (G)

Department of Pharmaceutical Sciences , Università degli Studi di Milano , Via Mangiagalli 25 , 20133 Milan , Italy.
ORCID: 0000-0002-3939-5172

Giulio Rastelli (G)

Department of Life Sciences , University of Modena and Reggio Emilia , Via Campi 103 , 41125 Modena , Italy.
ORCID: 0000-0002-2474-0607

Carlo Riva (C)

Drug Discovery Department , Recordati S.p.A. , Via M. Civitali 1 , 20148 Milan , Italy.

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Régulation allostérique › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Composés chimiques organiques › Amides › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Eucaryotes › Animaux › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Pharmacocinétique › Biodisponibilité › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules CHO › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Composés chimiques organiques › Acides carboxyliques › Acides acycliques › Carbamates › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Arvicolinae › Cricetinae › Cricetulus › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents des acides aminés excitateurs › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs métabotropes au glutamate › Récepteur-5 métabotropique du glutamate › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Sulfones › Sulfonamides › Evaluation of Amides, Carbamates,...
questionsmedicales.fr › Composés chimiques organiques › Amides › Urée › Evaluation of Amides, Carbamates,...