Results 171 to 180 of about 13,446 (217)

Suicidal Ideation Following a Single Dose of Melatonin in a Patient With Major Depressive Disorder: A Case Report. [PDF]

Clin Case Rep
Badrfam R, Zandifar A.
europepmc   +1 more source

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The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators

European Journal of Medicinal Chemistry, 2023
Melatonin, a neurohormone secreted by the pineal gland and regulated by the suprachiasmatic nucleus (SCN) of the hypothalamus, is synthesized and directly released into the cerebrospinal fluid (CSF) of the third ventricle (3rdv), where it undergoes rapid absorption by surrounding tissues to exert its physiological function.
Yueqin, Feng, Xiaowen, Jiang, Wenwu, Liu, Hongyuan, Lu   +3 more
openaire   +2 more sources

Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2004
A series of tetrahydroisoquinolines has yielded potent MT(2) receptor antagonists, which are selective versus the MT(1) receptor.
George N, Karageorge, Stephen, Bertenshaw, Lawrence, Iben, Cen, Xu, Nathan, Sarbin, Anthony, Gentile, Gene M, Dubowchik   +6 more
openaire   +2 more sources

Investigational Selective Melatoninergic Ligands for Receptor Subtype MT2

Mini-Reviews in Medicinal Chemistry, 2013
Melatonin, an endogenous ligand for melatonin receptor, plays an important role in modulating various physiological activities through acting on different subtypes MT1, MT2 or the binding site MT3. The distinct roles of the receptor subtypes provide great potential for receptor-specific pharmacological agents. Melatonin has no subtypeselectivity, so it
Ning, Wan, Fang-Fang, Zhang, Jia, Ju, Dao-Zhou, Liu, Si-Yuan, Zhou, Bang-Le, Zhang   +5 more
openaire   +2 more sources

Mutagenesis studies of the human MT2 melatonin receptor

Biochemical Pharmacology, 2003
Melatonin mediates its physiological effects through activation of high affinity G protein-coupled receptors. The vertebrate MT(1), MT(2) and Mel(1c) melatonin receptors are molecularly and pharmacologically distinct. Three molecular models of melatonin recognition for the MT(1) and/or Mel(1c) melatonin receptors have been proposed.
Matthew J, Gerdin, Faika, Mseeh, Margarita L, Dubocovich   +2 more
openaire   +2 more sources

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

Behavioural Brain Research, 2013
The neurohormone melatonin activates two G-protein coupled receptors, MT1 and MT2. Melatonin is implicated in circadian rhythms and sleep regulation, but the role of its receptors remains to be defined. We have therefore characterized the spontaneous vigilance states in wild-type (WT) mice and in three different types of transgenic mice: mice with ...
Comai S., Ochoa-Sanchez R., Gobbi G.
openaire   +2 more sources

Preferential Formation of MT1/MT2 Melatonin Receptor Heterodimers with Distinct Ligand Interaction Properties Compared with MT2 Homodimers

Molecular Pharmacology, 2004
Heterodimerization has been documented for several members of the G protein-coupled receptor (GPCR) superfamily, including the closely related MT(1) and MT(2) melatonin receptors. However, the relative abundance of hetero-versus homodimers and the specific properties, which can be attributed to each form, are difficult to determine.
Mohammed A, Ayoub, Angélique, Levoye, Philippe, Delagrange, Ralf, Jockers   +3 more
openaire   +2 more sources

Homology modeling of MT1 and MT2 receptors

European Journal of Medicinal Chemistry, 2008
Melatonin is a neurohormone synthesized and secreted mainly during the dark period of the circadian cycle by the pineal gland. It has already been proved to be involved in a number of chronobiological processes, most of them being mediated by its membranar receptors MT1 and MT2.
Farce, Amaury, Chugunov, Anton O., Logé, Cédric, Sabaouni, Ahmed, Yous, Said, Dilly, Sébastien, Renault, Nicolas, Vergoten, Gérard, Efremov, Roman G., Lesieur, Daniel, Chavatte, Philippe   +10 more
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Strategies Leading To MT2 Selective Melatonin Receptor Antagonists

2003
Studies of the physiological actions of melatonin have been hindered by the lack of specific, potent and subtype selective agonists and antagonists. This paper reviews our progress in developing subtype selective melatonin antagonists. Evidence is presented suggesting the structural features conferring MT2 selective antagonism.
SPADONI, GILBERTO, BEDINI, ANNALIDA, PIERSANTI, GIOVANNI, MOR M., RIVARA S., TARZIA, GIORGIO   +5 more
openaire   +3 more sources

Impaired hippocampal long-term potentiation in melatonin MT2 receptor-deficient mice

Neuroscience Letters, 2006
The pineal product melatonin that acts on specific melatonin receptors has been implicated in pathobiological mechanisms of neuropsychiatric disorders including Alzheimer's disease. We used mice lacking melatonin MT(2) receptors (MT(2) knockouts) to investigate the role of these receptors in synaptic plasticity and learning-dependent behavior. In field
John, Larson, Ruth E, Jessen, Tolga, Uz, Ahmet D, Arslan, Murat, Kurtuncu, Marta, Imbesi, Hari, Manev   +6 more
openaire   +2 more sources