Melatonin receptor ligands: A pharmaco‐chemical perspective

Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

(2020) Reed M. Stein et al.   NATURE

Structure-based discovery of potent and selective melatonin receptor agonists

(2020) Nilkanth Patel et al.   eLife

Structure-Based Virtual Screening Accelerates GPCR Drug Discovery

(2020) Lei Liu et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

O-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors

(2019) Angeliki Karamitri et al.   BIOORGANIC CHEMISTRY

XFEL structures of the human MT2 melatonin receptor reveal the basis of subtype selectivity

(2019) Linda C. Johansson et al.   NATURE

Structural basis of ligand recognition at the human MT1 melatonin receptor

(2019) Benjamin Stauch et al.   NATURE

Pharmacological, Mechanistic, and Pharmacokinetic Assessment of Novel Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs

(2019) Mahmud Hasan et al.   MOLECULAR PHARMACOLOGY

Melatonin receptor structures shed new light on melatonin research

(2019) Erika Cecon et al.   JOURNAL OF PINEAL RESEARCH

Structural insights into melatonin receptors

(2019) Benjamin Stauch et al.   FEBS Journal

Identification of a novel melatonin‐binding nuclear receptor: Vitamin D receptor

(2019) Nan Fang et al.   JOURNAL OF PINEAL RESEARCH

Melatonin Target Proteins: Too Many or Not Enough?

(2019) Lei Liu et al.   Frontiers in Endocrinology

Indole-based melatonin analogues: Synthetic approaches and biological activity

(2019) Su-Yan Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of magnolol derivatives as melatonergic receptor agonists with potential use in depression

(2018) Tong-Hua Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tetrahydroquinoline Ring as a Versatile Bioisostere of Tetralin for Melatonin Receptor Ligands

(2018) Silvia Rivara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of the Mel1c melatoninergic receptor in platypus (Ornithorhynchus anatinus)

(2018) Célia Gautier et al.   PLoS One

Identification of Bivalent Ligands with Melatonin Receptor Agonist and Fatty Acid Amide Hydrolase (FAAH) Inhibitory Activity That Exhibit Ocular Hypotensive Effect in the Rabbit

(2018) Gilberto Spadoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Activity of Hydrogen Peroxide Responsive Arylboronate Melatonin Hybrids

(2018) Annalida Bedini et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Is There Sufficient Evidence that the Melatonin Binding Site MT3 Is Quinone Reductase 2?

(2018) Jean A. Boutin et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Detection of recombinant and endogenous mouse melatonin receptors by monoclonal antibodies targeting the C-terminal domain

(2018) Erika Cecon et al.   JOURNAL OF PINEAL RESEARCH

New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation

(2017) Elodie Landagaray et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT 1 /MT 2 ) and serotoninergic (5-HT 2C ) dual ligands

(2017) Romain Duroux et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Agomelatine for the treatment of generalized anxiety disorder

(2017) Massimiliano Buoli et al.   EXPERT OPINION ON PHARMACOTHERAPY

New MT2 Melatonin Receptor-Selective Ligands: Agonists and Partial Agonists

(2017) Jean Boutin et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists

(2017) Xiu-Juan Yin et al.   JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH

Dual role of mitochondria in producing melatonin and driving GPCR signaling to block cytochrome c release

(2017) Yalikun Suofu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Update on melatonin receptors: IUPHAR Review 20

(2016) Ralf Jockers et al.   BRITISH JOURNAL OF PHARMACOLOGY

Tasimelteon: A Review in Non-24-Hour Sleep-Wake Disorder in Totally Blind Individuals

(2016) Gillian M. Keating   CNS DRUGS

Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives

(2016) Elodie Landagaray et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity

(2016) Audrey Couhert et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Systematic Study of Effects of Structural Modifications on the Aqueous Solubility of Drug-like Molecules

(2016) José A. Cisneros et al.   ACS Medicinal Chemistry Letters

Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2 melatonin receptors

(2016) G. Viault et al.   RSC Advances

Curcumin/Melatonin Hybrid 5-(4-Hydroxy-phenyl)-3-oxo-pentanoic Acid [2-(5-Methoxy-1H-indol-3-yl)-ethyl]-amide Ameliorates AD-Like Pathology in the APP/PS1 Mouse Model

(2015) Gorka Gerenu et al.   ACS Chemical Neuroscience

New coumarin-based fluorescent melatonin ligands. Design, synthesis and pharmacological characterization

(2015) Mario de la Fuente Revenga et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II)

(2015) Mohamed Ettaoussi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Quinone reductase 2 as a promising target of melatonin therapeutic actions

(2015) Jean A Boutin   EXPERT OPINION ON THERAPEUTIC TARGETS

Even free radicals should follow some rules: A Guide to free radical research terminology and methodology

(2015) Henry Jay Forman et al.   FREE RADICAL BIOLOGY AND MEDICINE

Highly Potent and Selective MT2 Melatonin Receptor Full Agonists from Conformational Analysis of 1-Benzyl-2-acylaminomethyl-tetrahydroquinolines

(2015) Gilberto Spadoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel difluoroacetamide analogues of agomelatine and melatonin: probing the melatonin receptors for MT1 selectivity

(2015) Darius P. Zlotos et al.   MedChemComm

Discovery of 5-(4-Hydroxyphenyl)-3-oxo-pentanoic Acid [2-(5-Methoxy-1H-indol-3-yl)-ethyl]-amide as a Neuroprotectant for Alzheimer’s Disease by Hybridization of Curcumin and Melatonin

(2014) Jeremy E. Chojnacki et al.   ACS Chemical Neuroscience

New melatonin (MT1/MT2) ligands: Design and synthesis of (8,9-dihydro-7H-furo[3,2-f]chromen-1-yl) derivatives

(2014) Elodie Landagaray et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Benzocyclobutane, Benzocycloheptane and Heptene Derivatives as Melatonin Agonists and Antagonists

(2014) Andrew Tsotinis et al.   ChemMedChem

Recombinant Human Melatonin Receptor MT1 Isolated in Mixed Detergents Shows Pharmacology Similar to That in Mammalian Cell Membranes

(2014) Christel Logez et al.   PLoS One

Synthesis and Functional Characterization of Substituted Isoquinolinones as MT2-Selective Melatoninergic Ligands

(2014) Yueqing Hu et al.   PLoS One

Melatonin MT1and MT2receptors display different molecular pharmacologies only in the G-protein coupled state

(2013) Céline Legros et al.   BRITISH JOURNAL OF PHARMACOLOGY

Synthesis and Pharmacological Evaluation of a series of the Agomelatine Analogues as Melatonin MT1/MT2Agonist and 5-HT2CAntagonist

(2013) Mohamed Ettaoussi et al.   ChemMedChem

Characterization of Substituted Phenylpropylamides as Highly Selective Agonists at the Melatonin MT2 Receptor

(2013) King H. Chan et al.   CURRENT MEDICINAL CHEMISTRY

How do nutritional antioxidants really work: Nucleophilic tone and para-hormesis versus free radical scavenging in vivo

(2013) Henry J. Forman et al.   FREE RADICAL BIOLOGY AND MEDICINE

New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors

(2013) Céline Legros et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

MT1 and MT2 Melatonin Receptors: Ligands, Models, Oligomers, and Therapeutic Potential

(2013) Darius. P. Zlotos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Original Design of Fluorescent Ligands by Fusing BODIPY and Melatonin Neurohormone

(2013) Jérémy Thireau et al.   ACS Medicinal Chemistry Letters

Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT2-selective melatonin agonists: Improving metabolic stability

(2012) Yueqing Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of new N-(arylcyclopropyl)acetamides and N-(arylvinyl)acetamides as conformationally-restricted ligands for melatonin receptors

(2012) Laurence Morellato et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

MT1-Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation ofN-{[(3-O-Substituted)anilino]alkyl}amides

(2012) Silvia Rivara et al.   ChemMedChem

Recent Progress in the Development of Agonists and Antagonists for Melatonin Receptors

(2012) D. P. Zlotos   CURRENT MEDICINAL CHEMISTRY

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I)

(2012) Mohamed Ettaoussi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel Conformationally Constrained Analogues of Agomelatine as New Melatoninergic Ligands

(2012) Marouan Rami et al.   MOLECULES

Pharmacokinetics, oral bioavailability and metabolism of a novel isoquinolinone-based melatonin receptor agonist in rats

(2012) Jing Zhu et al.   XENOBIOTICA

N-Acetyl-5-arylalkoxytryptamine Analogs: Probing the Melatonin Receptors for MT1-Selectivity

(2011) Christian Markl et al.   ARCHIV DER PHARMAZIE

Bivalent ligand approach on N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide: Synthesis, binding affinity and intrinsic activity for MT1 and MT2 melatonin receptors

(2011) Gilberto Spadoni et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists

(2011) Matthieu Jeanty et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands

(2011) Christophe Mésangeau et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of 2-phenylimidazo[1,2-a]pyridines as a novel class of melatonin receptor ligands

(2011) Saïd El Kazzouli et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of a Novel Series of Tricyclic Dihydrofuran Derivatives: Discovery of 8,9-Dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as Melatonin Receptor (MT1/MT2) Ligands

(2011) Tatsuki Koike et al.   JOURNAL OF MEDICINAL CHEMISTRY

1,6-Dihydro-2H-indeno[5,4-b]furan Derivatives: Design, Synthesis, and Pharmacological Characterization of a Novel Class of Highly Potent MT2-Selective Agonists

(2011) Tatsuki Koike et al.   JOURNAL OF MEDICINAL CHEMISTRY

Melatonin has membrane receptor-independent hypnotic action on neurons: an hypothesis

(2011) James E. Jan et al.   JOURNAL OF PINEAL RESEARCH

2-[(1,3-Dihydro-2H-isoindol-2-yl)methyl]melatonin – a novel MT2-selective melatonin receptor antagonist

(2011) David Heckman et al.   MedChemComm

Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT1 melatoninergic ligands

(2010) Christophe Mésangeau et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors

(2010) Alessia Carocci et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT2-selective melatonin ligands

(2010) Yueqing Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands

(2010) Guiying Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent advances in the development of melatonin MT1and MT2receptor agonists

(2010) Marco Mor et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

High-throughput screening assay for new ligands at human melatonin receptors

(2009) Jian-hua Yan et al.   ACTA PHARMACOLOGICA SINICA

Synthesis and pharmacological evaluation of 1,2,3,4-tetrahydropyrazino[1,2-a]indole and 2-[(phenylmethylamino)methyl]-1H-indole analogues as novel melatoninergic ligands

(2009) Christian Markl et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II

(2009) Sophie Durieux et al.   BIOORGANIC & MEDICINAL CHEMISTRY

N-(Anilinoethyl)amides: Design and Synthesis of Metabolically Stable, Selective Melatonin Receptor Ligands

(2009) Silvia Rivara et al.   ChemMedChem

2-[(2,3-Dihydro-1H-indol-1-yl)methyl]melatonin Analogues: A Novel Class of MT2-Selective Melatonin Receptor Antagonists

(2009) Darius P. Zlotos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and pharmacological evaluation of pentacyclic 6a,7-dihydrodiindole and 2,3-dihydrodiindole derivatives as novel melatoninergic ligands

(2008) Mohamed I. Attia et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of 3-phenylnaphthalenic derivatives as new selective MT2 melatoninergic ligands

(2008) Sophie Poissonnier-Durieux et al.   BIOORGANIC & MEDICINAL CHEMISTRY