Update on melatonin receptors: IUPHAR Review 20

MT1and MT2Melatonin Receptors: A Therapeutic Perspective

(2016) Jiabei Liu et al.   Annual Review of Pharmacology and Toxicology

Consequences of long-term treatment with agomelatine on depressive-like behavior and neurobiological abnormalities in pinealectomized rats

(2016) Jana Tchekalarova et al.   BEHAVIOURAL BRAIN RESEARCH

The RelA/cRel nuclear factor-κB (NF-κB) dimer, crucial for inflammation resolution, mediates the transcription of the key enzyme in melatonin synthesis in RAW 264.7 macrophages

(2016) Sandra Marcia Muxel et al.   JOURNAL OF PINEAL RESEARCH

Melatonin receptor activation increases glutamatergic synaptic transmission in the rat medial lateral habenula

(2016) Katherine M. Evely et al.   SYNAPSE

Melatonin Signaling Controls the Daily Rhythm in Blood Glucose Levels Independent of Peripheral Clocks

(2016) Sharon Owino et al.   PLoS One

The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: Transporters

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: Voltage-gated ion channels

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: Enzymes

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Melatonin Contributes to the Seasonality of Multiple Sclerosis Relapses

(2015) Mauricio F. Farez et al.   CELL

Photoperiod Programs Dorsal Raphe Serotonergic Neurons and Affective Behaviors

(2015) Noah H. Green et al.   CURRENT BIOLOGY

Amyloid β peptide directly impairs pineal gland melatonin synthesis and melatonin receptor signaling through the ERK pathway

(2015) Erika Cecon et al.   FASEB JOURNAL

Neuroendocrine control of photoperiodic changes in immune function

(2015) Zachary M. Weil et al.   FRONTIERS IN NEUROENDOCRINOLOGY

Melatonin Stimulates Dendrite Formation and Complexity in the Hilar Zone of the Rat Hippocampus: Participation of the Ca++/Calmodulin Complex

(2015) Aline Domínguez-Alonso et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Convergence of Melatonin and Serotonin (5-HT) Signaling at MT2/5-HT2CReceptor Heteromers

(2015) Maud Kamal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

60 YEARS OF NEUROENDOCRINOLOGY: Regulation of mammalian neuroendocrine physiology and rhythms by melatonin

(2015) Jonathan D Johnston et al.   JOURNAL OF ENDOCRINOLOGY

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 N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential

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

Melatonin enhances L-DOPA therapeutic effects, helps to reduce its dose, and protects dopaminergic neurons in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced parkinsonism in mice

(2015) Amit Naskar et al.   JOURNAL OF PINEAL RESEARCH

Melatonin attenuatesLeishmania (L.) amazonensisinfection by modulating arginine metabolism

(2015) Maria Fernanda Laranjeira-Silva et al.   JOURNAL OF PINEAL RESEARCH

Melatonin uptake through glucose transporters: a new target for melatonin inhibition of cancer

(2015) David Hevia et al.   JOURNAL OF PINEAL RESEARCH

Protein interactome mining defines melatonin MT1receptors as integral component of presynaptic protein complexes of neurons

(2015) Abla Benleulmi-Chaachoua et al.   JOURNAL OF PINEAL RESEARCH

Prophylactic melatonin significantly reduces Alzheimer’s neuropathology and associated cognitive deficits independent of antioxidant pathways in AβPPswe/PS1 mice

(2015) G. O’Neal-Moffitt et al.   Molecular Neurodegeneration

Melatonin as a Potent and Inducible Endogenous Antioxidant: Synthesis and Metabolism

(2015) Dun-Xian Tan et al.   MOLECULES

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

(2015) Yanyong Kang et al.   NATURE

Exogenous melatonin for sleep disorders in neurodegenerative diseases: a meta-analysis of randomized clinical trials

(2015) Wei Zhang et al.   NEUROLOGICAL SCIENCES

Tasimelteon: A selective and unique receptor binding profile

(2015) Christian Lavedan et al.   NEUROPHARMACOLOGY

The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands

(2015) Christopher Southan et al.   NUCLEIC ACIDS RESEARCH

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

(2015) Darius P. Zlotos et al.   MedChemComm

Understanding melatonin receptor pharmacology: Latest insights from mouse models, and their relevance to human disease

(2014) Gianluca Tosini et al.   BIOESSAYS

The MT2 receptor stimulates axonogenesis and enhances synaptic transmission by activating Akt signaling

(2014) D Liu et al.   CELL DEATH AND DIFFERENTIATION

The Role of Melatonin in Multiple Sclerosis, Huntington's Disease and Cerebral Ischemia

(2014) Begona Escribano et al.   CNS & Neurological Disorders-Drug Targets

The melatonin analog 5-MCA-NAT increases endogenous dopamine levels by binding NRH:quinone reductase enzyme in the developing chick retina

(2014) Lucia de Fatima Sobral Sampaio et al.   INTERNATIONAL JOURNAL OF DEVELOPMENTAL NEUROSCIENCE

Melatonin from Cerebrospinal Fluid but Not from Blood Reaches Sheep Cerebral Tissues Under Physiological Conditions

(2014) C. Legros et al.   JOURNAL OF NEUROENDOCRINOLOGY

Computational Study on the Kinetics and Mechanism of the Carbaryl + OH Reaction

(2014) Claudia Zavala-Oseguera et al.   JOURNAL OF PHYSICAL CHEMISTRY A

Melatonin promotes the acquisition of neural identity through extracellular-signal-regulated kinases 1/2 activation

(2014) Xueran Chen et al.   JOURNAL OF PINEAL RESEARCH

Melatonin attenuates neutrophil inflammation and mucus secretion in cigarette smoke-induced chronic obstructive pulmonary diseases via the suppression of Erk-Sp1 signaling

(2014) In-Sik Shin et al.   JOURNAL OF PINEAL RESEARCH

Promising Role of Melatonin as Neuroprotectant in Neurodegenerative Pathology

(2014) Neeraj Joshi et al.   MOLECULAR NEUROBIOLOGY

Genetic deletion of MT1/MT2 melatonin receptors enhances murine cognitive and motor performance

(2014) G. O’Neal-Moffitt et al.   NEUROSCIENCE

Genetic deletion of the MT1 or MT2 melatonin receptors abrogates methamphetamine-induced reward in C3H/HeN mice

(2014) Shannon J. Clough et al.   PHYSIOLOGY & BEHAVIOR

N1-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors

(2014) Anne-Sophie Journé et al.   MedChemComm

Sleep–wake characterization of double MT1/MT2 receptor knockout mice and comparison with MT1 and MT2 receptor knockout mice

(2013) Stefano Comai et al.   BEHAVIOURAL BRAIN RESEARCH

Automated video analysis system reveals distinct diurnal behaviors in C57BL/6 and C3H/HeN mice

(2013) E.B. Adamah-Biassi et al.   BEHAVIOURAL BRAIN RESEARCH

Selective protection of the cerebellum against intracerebroventricular LPS is mediated by local melatonin synthesis

(2013) Luciana Pinato et al.   Brain Structure & Function

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

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

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

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

Immune-Pineal Axis: Nuclear Factor κB (NF-kB) Mediates the Shift in the Melatonin Source from Pinealocytes to Immune Competent Cells

(2013) Regina Markus et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Melatonin: Buffering the Immune System

(2013) Antonio Carrillo-Vico et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Structure-Based Virtual Screening of MT2 Melatonin Receptor: Influence of Template Choice and Structural Refinement

(2013) Daniele Pala et al.   Journal of Chemical Information and Modeling

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

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

Reciprocal interaction between melatonin receptors (Mel1a, Mel1b, and Mel1c) and androgen receptor (AR) expression in immunoregulation of a seasonally breeding bird, Perdicula asiatica: Role of photoperiod

(2013) S.K. Yadav et al.   JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY

Melatonin synthesis in human colostrum mononuclear cells enhances dectin-1-mediated phagocytosis by mononuclear cells

(2013) Marco A. Pires-Lapa et al.   JOURNAL OF PINEAL RESEARCH

Fish oil, melatonin and vitamin E attenuates midbrain cyclooxygenase-2 activity and oxidative stress after the administration of 1-methyl-4-phenyl-1,2,3,6- tetrahydropyridine

(2013) Genaro Gabriel Ortiz et al.   METABOLIC BRAIN DISEASE

Minireview: Toward the Establishment of a Link between Melatonin and Glucose Homeostasis: Association of Melatonin MT2Receptor Variants with Type 2 Diabetes

(2013) Angeliki Karamitri et al.   MOLECULAR ENDOCRINOLOGY

Disease-modified glycogen synthase kinase-3β intervention by melatonin arrests the pathology and memory deficits in an Alzheimer's animal model

(2013) Cai-Xia Peng et al.   NEUROBIOLOGY OF AGING

Melatonin inhibits the caspase-1/cytochrome c/caspase-3 cell death pathway, inhibits MT1 receptor loss and delays disease progression in a mouse model of amyotrophic lateral sclerosis

(2013) Yi Zhang et al.   NEUROBIOLOGY OF DISEASE

Heteromeric MT1/MT2 Melatonin Receptors Modulate Photoreceptor Function

(2013) K. Baba et al.   Science Signaling

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

The Endogenous Melatonin (MT) Signal Facilitates Reentrainment of the Circadian System to Light-Induced Phase Advances by Acting Upon MT2 Receptors

(2012) Martina Pfeffer et al.   CHRONOBIOLOGY INTERNATIONAL

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

Melatonin: An underappreciated player in retinal physiology and pathophysiology

(2012) Gianluca Tosini et al.   EXPERIMENTAL EYE RESEARCH

Genetic deletion of MT1and MT2melatonin receptors differentially abrogates the development and expression of methamphetamine-induced locomotor sensitization during the day and the night in C3H/HeN mice

(2012) Anthony J. Hutchinson et al.   JOURNAL OF PINEAL RESEARCH

An integrated map of genetic variation from 1,092 human genomes

(2012)   NATURE

Rare MTNR1B variants impairing melatonin receptor 1B function contribute to type 2 diabetes

(2012) Amélie Bonnefond et al.   NATURE GENETICS

NF-κB Drives the Synthesis of Melatonin in RAW 264.7 Macrophages by Inducing the Transcription of the Arylalkylamine-N-Acetyltransferase (AA-NAT) Gene

(2012) Sandra Marcia Muxel et al.   PLoS One

An Abundance of Rare Functional Variants in 202 Drug Target Genes Sequenced in 14,002 People

(2012) M. R. Nelson et al.   SCIENCE

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

Application of the bridgehead fragments for the design of conformationally restricted melatonin analogues

(2011) Olga N. Zefirova et al.   BIOORGANIC 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

Promotion of Non-Rapid Eye Movement Sleep and Activation of Reticular Thalamic Neurons by a Novel MT2 Melatonin Receptor Ligand

(2011) R. Ochoa-Sanchez et al.   JOURNAL OF NEUROSCIENCE

The Melatonin MT1 Receptor Axis Modulates Mutant Huntingtin-Mediated Toxicity

(2011) X. Wang et al.   JOURNAL OF NEUROSCIENCE

Genetic variations of the melatonin pathway in patients with attention-deficit and hyperactivity disorders

(2011) Pauline Chaste et al.   JOURNAL OF PINEAL RESEARCH

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Removal of melatonin receptor type 1 increases intraocular pressure and retinal ganglion cells death in the mouse

(2011) Susana Alcantara-Contreras et al.   NEUROSCIENCE LETTERS

Localization of Melatonin Receptor 1 in Mouse Retina and Its Role in the Circadian Regulation of the Electroretinogram and Dopamine Levels

(2011) Anamika Sengupta et al.   PLoS One

Asymmetry of GPCR oligomers supports their functional relevance

(2011) Pascal Maurice et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Mode of action of agomelatine: Synergy between melatonergic and 5-HT2Creceptors

(2011) Giorgio Racagni et al.   WORLD JOURNAL OF BIOLOGICAL PSYCHIATRY

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

(2011) David Heckman et al.   MedChemComm

Ligand-Induced Modulation of the Free-Energy Landscape of G Protein-Coupled Receptors Explored by Adaptive Biasing Techniques

(2011) Davide Provasi et al.   PLoS Computational Biology

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

(2010) Christophe Mésangeau 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

Blocking of melatonin synthesis and MT1 receptor impairs the activation of Jurkat T cells

(2010) Patricia J. Lardone et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Circadian Periods of Sensitivity for Ramelteon on the onset of Running-wheel Activity and the Peak of Suprachiasmatic Nucleus Neuronal Firing Rhythms in C3H/HeN Mice

(2010) Oliver Rawashdeh et al.   CHRONOBIOLOGY INTERNATIONAL

Clinical Aspects of Melatonin Intervention in Alzheimers Disease Progression

(2010) Daniel P. Cardinali et al.   Current Neuropharmacology

MTNR1B G24E Variant Associates With BMI and Fasting Plasma Glucose in the General Population in Studies of 22,142 Europeans

(2010) E. A. Andersson et al.   DIABETES

Molecular and cellular pharmacological properties of 5-methoxycarbonylamino-N-acetyltryptamine (MCA-NAT): a nonspecific MT3 ligand

(2010) Ludwig Vincent et al.   JOURNAL OF PINEAL RESEARCH

Erratum: Agomelatine, the first melatonergic antidepressant: discovery, characterization and development

(2010) Christian de Bodinat et al.   NATURE REVIEWS DRUG DISCOVERY

Removal of Melatonin Receptor Type 1 Induces Insulin Resistance in the Mouse

(2010) Susana Contreras-Alcantara et al.   Obesity

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

(2010) M. L. Dubocovich et al.   PHARMACOLOGICAL REVIEWS

Identification of Pathway-Biased and Deleterious Melatonin Receptor Mutants in Autism Spectrum Disorders and in the General Population

(2010) Pauline Chaste et al.   PLoS One

Long-Lasting Priming of Endothelial Cells by Plasma Melatonin Levels

(2010) Eduardo Koji Tamura et al.   PLoS One

RESPONSE OF MELATONIN RECEPTOR MT1 IN SPLEEN OF A TROPICAL INDIAN RODENT,FUNAMBULUS PENNANTI,TO NATURAL SOLAR INSOLATION AND DIFFERENT PHOTOPERIODIC CONDITIONS

(2009) Sanjukta Lahiri et al.   CHRONOBIOLOGY INTERNATIONAL

Antagonism of serotonergic 5-HT2A/2Creceptors: mutual improvement of sleep, cognition and mood?

(2009) H.-P. Landolt et al.   EUROPEAN JOURNAL OF NEUROSCIENCE

Loss of melatonin signalling and its impact on circadian rhythms in mouse organs regulating blood glucose

(2009) Eckhard Mühlbauer et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

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

Melatonin Transmits Photoperiodic Signals through the MT1 Melatonin Receptor

(2009) S. Yasuo et al.   JOURNAL OF NEUROSCIENCE

5-MCA-NAT does not act through NQO2 to reduce intraocular pressure in New-Zealand white rabbit

(2009) Pilar Alarma-Estrany et al.   JOURNAL OF PINEAL RESEARCH

Protection against cognitive deficits and markers of neurodegeneration by long-term oral administration of melatonin in a transgenic model of Alzheimer disease

(2009) James M. Olcese et al.   JOURNAL OF PINEAL RESEARCH

Sleep-promoting action of IIK7, a selective MT2 melatonin receptor agonist in the rat

(2009) Simon P. Fisher et al.   NEUROSCIENCE LETTERS

Melatonin modulates visual function and cell viability in the mouse retina via the MT1 melatonin receptor

(2009) K. Baba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?

(2008) R Jockers et al.   BRITISH JOURNAL OF PHARMACOLOGY

Homology modeling of MT1 and MT2 receptors

(2008) Amaury Farce et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Involvement of the cGMP pathway in mediating the insulin-inhibitory effect of melatonin in pancreatic β-cells

(2008) Ina Stumpf et al.   JOURNAL OF PINEAL RESEARCH

Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials

(2008) Shantha MW Rajaratnam et al.   LANCET

A Generic Approach for the Purification of Signaling Complexes That Specifically Interact with the Carboxyl-terminal Domain of G Protein-coupled Receptors

(2008) Pascal Maurice et al.   MOLECULAR & CELLULAR PROTEOMICS

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE

Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion

(2008) Valeriya Lyssenko et al.   NATURE GENETICS

Variants in MTNR1B influence fasting glucose levels

(2008) Inga Prokopenko et al.   NATURE GENETICS

A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk

(2008) Nabila Bouatia-Naji et al.   NATURE GENETICS

Structural diversity in the RGS domain and its interaction with heterotrimeric G protein  -subunits

(2008) M. Soundararajan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA