Carbachol dimers with primary carbamate groups as homobivalent modulators of muscarinic receptors.

Animals CHO Cells Carbachol / chemistry Cricetulus Cyclic AMP / metabolism Dimerization Extracellular Signal-Regulated MAP Kinases / metabolism Guanosine 5'-O-(3-Thiotriphosphate) / metabolism Humans Kinetics Molecular Docking Simulation Molecular Structure Muscarinic Agonists / chemistry Muscarinic Antagonists / chemistry Phosphorylation Protein Binding Receptors, Muscarinic / drug effects Signal Transduction Structure-Activity Relationship
Acethylcholine chloride Allosteric modulation Atropine sulphate Carbachol chloride Carbachol dimers Gallamine triethiodide Hexamethonium chloride McN-A-343 chloride Muscarinic acetylcholine receptor (mAChR) PubChem CID: 5831 PubChem CID: 5926 PubChem CID: 6060 PubChem CID: 6172 PubChem CID: 64663 PubChem CID: 93550

Journal

European journal of pharmacology
ISSN: 1879-0712
Titre abrégé: Eur J Pharmacol
Pays: Netherlands
ID NLM: 1254354

Informations de publication

Date de publication:
15 Sep 2020
Historique:
received: 09 10 2019
revised: 23 03 2020
accepted: 08 05 2020
pubmed: 14 6 2020
medline: 19 5 2021
entrez: 14 6 2020
Statut: ppublish

Résumé

Although agonists and antagonists of muscarinic receptors have been known for long time, there is renewed interest in compounds (such as allosteric or bitopic ligands, or biased agonists) able to differently and selectively modulate these receptors. As a continuation of our previous research, we designed a new series of dimers of the well-known cholinergic agonist carbachol. The new compounds were tested on the five cloned human muscarinic receptors (hM

Identifiants

DOI: 10.1016/j.ejphar.2020.173183 PMID: 32534072
pubmed: 32534072
pii: S0014-2999(20)30275-2
doi: 10.1016/j.ejphar.2020.173183
pii:
doi:

Substances chimiques

Muscarinic Agonists 0
Muscarinic Antagonists 0
Receptors, Muscarinic 0
Guanosine 5'-O-(3-Thiotriphosphate) 37589-80-3
Carbachol 8Y164V895Y
Cyclic AMP E0399OZS9N
Extracellular Signal-Regulated MAP Kinases EC 2.7.11.24

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

173183

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Auteurs

Rosanna Matucci (R)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmacology and Toxicology, University of Florence, Viale G. Pieraccini 6, 50139, Firenze, Italy. Electronic address: rosanna.matucci@unifi.it.

Cristina Bellucci (C)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

Maria Vittoria Martino (MV)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

Marta Nesi (M)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmacology and Toxicology, University of Florence, Viale G. Pieraccini 6, 50139, Firenze, Italy.

Dina Manetti (D)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

Jessica Welzel (J)

Department of Pharmacology & Toxicology, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Ulrike Bartz (U)

Department of Natural Sciences, H-BRS University of Applied Sciences, von-Liebig-Str. 20, 53359, Rheinbach, Germany.

Janine Holze (J)

Department of Pharmacology & Toxicology, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Christian Tränkle (C)

Department of Pharmacology & Toxicology, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Klaus Mohr (K)

Department of Pharmacology & Toxicology, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Angelica Mazzolari (A)

Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133, Milano, Italy.

Giulio Vistoli (G)

Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133, Milano, Italy.

Silvia Dei (S)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

Elisabetta Teodori (E)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

Maria Novella Romanelli (MN)

Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules CHO › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Composés chimiques organiques › Composés onium › Composés d'ammonium quaternaire › Choline › Carbachol › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Arvicolinae › Cricetinae › Cricetulus › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléotides › Ribonucléotides › Nucléotides adényliques › AMP cyclique › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Métabolisme › Dimérisation › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › Mitogen-Activated Protein Kinases › Extracellular Signal-Regulated MAP Kinases › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléotides › Thionucléotides › Guanosine 5'-O-(3-thiotriphosphate) › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Agonistes cholinergiques › Agonistes muscariniques › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Antagonistes cholinergiques › Antagonistes muscariniques › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Métabolisme › Phosphorylation › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs cholinergiques › Récepteur muscarinique › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Transduction du signal › Carbachol dimers with primary carbamate groups...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Carbachol dimers with primary carbamate groups...