[HTML][HTML] Structural Basis for Agonistic Activity and Selectivity toward Melatonin Receptors hMT1 and hMT2
M Cantarini, D Rusciano, R Amato, A Canovai… - International Journal of …, 2023 - mdpi.com
Glaucoma, a major ocular neuropathy originating from a progressive degeneration of retinal
ganglion cells, is often associated with increased intraocular pressure (IOP). Daily IOP …
ganglion cells, is often associated with increased intraocular pressure (IOP). Daily IOP …
2-Arylmelatonin analogues: Probing the 2-phenyl binding pocket of melatonin MT1 and MT2 receptors
In crystal structures of melatonin MT 1 and MT 2 receptors, a lipophilic subpocket has been
characterized which accommodates the phenyl ring of the potent agonist 2-phenylmelatonin …
characterized which accommodates the phenyl ring of the potent agonist 2-phenylmelatonin …
MT1‐Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation of N‐{[(3‐O‐Substituted)anilino]alkyl} …
The design of compounds selective for the MT1 melatonin receptor is still a challenging task
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
Analysis of Structure−Activity Relationships for MT2 Selective Antagonists by Melatonin MT1 and MT2 Receptor Models
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II)
M Ettaoussi, B Peres, A Errazani, JA Boutin… - European Journal of …, 2015 - Elsevier
In this paper we report the investigation of C-3 and β-acetamide positions of agomelatine
analogues. Concomitant insertion of a hydroxymethyl in the β-acetamide position and …
analogues. Concomitant insertion of a hydroxymethyl in the β-acetamide position and …
[PDF][PDF] MT2 Selective melatonin receptor antagonists: design and structure-activity relationships
The neurohormone melatonin is involved in the regulation of many physiological functions,
in particular those related to circadian and seasonal rhythms. In mammals, melatonin …
in particular those related to circadian and seasonal rhythms. In mammals, melatonin …
Three-Dimensional Quantitative Structure−Activity Relationship Studies on Selected MT1 and MT2 Melatonin Receptor Ligands: Requirements for Subtype …
The three-dimensional quantitative structure− activity relationship comparative molecular
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
Synthesis, pharmacological characterization and QSAR studies on 2-substituted indole melatonin receptor ligands
A number of 6-methoxy-1-(2-propionylaminoethyl) indoles, carrying properly selected
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
Docking studies for melatonin receptors
HA Alkozi, JM Sanchez Montero… - Expert opinion on drug …, 2018 - Taylor & Francis
Introduction: Melatonin is a neurohormone that controls many relevant physiological
processes beyond the control of circadian rhythms. Melatonin's actions are carried out by …
processes beyond the control of circadian rhythms. Melatonin's actions are carried out by …
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 …