[HTML][HTML] Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties
C Herrera-Arozamena, M Estrada-Valencia… - European Journal of …, 2020 - Elsevier
New multi-target indole and naphthalene derivatives containing the oxadiazolone scaffold
as a bioisostere of the melatonin acetamido group have been developed. The novel …
as a bioisostere of the melatonin acetamido group have been developed. The novel …
New ligands at the melatonin binding site MT3
MF Boussard, S Truche, A Rousseau-Rojas… - European journal of …, 2006 - Elsevier
The third melatonin binding site, MT3 is a non-classical one since it is not a seven
transmembrane domains receptor, but an enzyme, quinone reductase 2. A major concern for …
transmembrane domains receptor, but an enzyme, quinone reductase 2. A major concern for …
Three-dimensional quantitative structure− activity relationship of melatonin receptor ligands: A comparative molecular field analysis study
S Sicsic, I Serraz, J Andrieux, B Brémont… - Journal of medicinal …, 1997 - ACS Publications
A three-dimensional quantitative structure− activity relationship using the comparative
molecular field analysis (CoMFA) paradigm applied to 57 melatonin receptor ligands …
molecular field analysis (CoMFA) paradigm applied to 57 melatonin receptor ligands …
Melatoninergic receptor agonists and antagonists: pharmacological aspects and therapeutic perspective
B Guardiola-Lemaitre - Annales Pharmaceutiques Francaises, 2005 - europepmc.org
Melatonin, or N-acetyl 5-methoxytryptamine, a neurohormone produced in the pineal gland
during periods of darkness, plays a key role in the regulation of circadian and seasonal …
during periods of darkness, plays a key role in the regulation of circadian and seasonal …
Recent developments in melatonin receptor ligands
M Mathé-Allainmat, J Andrieux… - Expert Opinion on …, 1997 - Taylor & Francis
In recent years, many physiological properties of melatonin have been described resulting in
much interest in the development of synthetic compounds possessing agonist or antagonist …
much interest in the development of synthetic compounds possessing agonist or antagonist …
Understanding melatonin receptor pharmacology: latest insights from mouse models, and their relevance to human disease
Melatonin, the neuro‐hormone synthesized during the night, has recently seen an
unexpected extension of its functional implications toward type 2 diabetes development …
unexpected extension of its functional implications toward type 2 diabetes development …
Reassessing the melatonin pharmacophore—Enantiomeric resolution, pharmacological activity, structure analysis, and molecular modeling of a constrained chiral …
3-(Acetylaminomethyl)-2-(ethoxycarbonyl)-6-methoxy-1, 3, 4, 5-tetrahydrobenzo [cd] indole
(2) is a rigid melatonin analogue that as a racemate displays about the same affinity and …
(2) is a rigid melatonin analogue that as a racemate displays about the same affinity and …
[PDF][PDF] Molecular pharmacology, regulation and function of mammalian melatonin receptors
ML Dubocovich, MA Rivera-Bermudez, MJ Gerdin… - Front …, 2003 - article.imrpress.com
Introduction 3. Melatonin receptors 3.1. MT1 and MT2 melatonin receptors 3.1. 1. Molecular
structure 3.1. 2. Pharmacology 3.1. 2.1. Efficacy, potency and affinity 3.1. 2.2. Ligand …
structure 3.1. 2. Pharmacology 3.1. 2.1. Efficacy, potency and affinity 3.1. 2.2. Ligand …
Bivalent ligand approach on N-{2-[(3-methoxyphenyl) methylamino] ethyl} acetamide: Synthesis, binding affinity and intrinsic activity for MT1 and MT2 melatonin …
We report the synthesis, binding properties and intrinsic activity at MT1 and MT2 melatonin
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …
Digging deep–structure–function relationships in the melatonin receptor family
P Barrett, S Conway, PJ Morgan - Journal of pineal research, 2003 - Wiley Online Library
The melatonin receptor family is a small group of receptors within the G protein‐coupled
receptor (GPCR) superfamily. The group comprises of three subtypes which bind melatonin …
receptor (GPCR) superfamily. The group comprises of three subtypes which bind melatonin …