Melatonin receptors: molecular pharmacology and signalling in the context of system bias
E Cecon, A Oishi, R Jockers - British journal of pharmacology, 2018 - Wiley Online Library
Melatonin, N‐acetyl‐5‐methoxytryptamine, an evolutionally old molecule, is produced by the
pineal gland in vertebrates, and it binds with high affinity to melatonin receptors, which are …
pineal gland in vertebrates, and it binds with high affinity to melatonin receptors, which are …
A new melatonin receptor ligand with mt1‐agonist and MT2‐antagonist properties
It has been difficult, so far, to obtain melatonin analogs possessing high selectivity for the
respective melatonin receptors, mt1 and MT2. In the present work, we report the synthesis …
respective melatonin receptors, mt1 and MT2. In the present work, we report the synthesis …
Molecular cloning and pharmacological characterization of rat melatonin MT1 and MT2 receptors
V Audinot, A Bonnaud, L Grandcolas… - Biochemical …, 2008 - Elsevier
In order to interpret the effects of melatonin ligands in rats, we need to determine their
activity at the receptor subtype level in the corresponding species. Thus, the rat melatonin …
activity at the receptor subtype level in the corresponding species. Thus, the rat melatonin …
Synthetic melatoninergic ligands: achievements and prospects
NV Kostiuk, MB Belyakova… - International …, 2014 - Wiley Online Library
Pineal hormone melatonin is widely used in the treatment of disorders of circadian rhythms.
The presence of melatonin receptors in various animal tissues motivates the use of this …
The presence of melatonin receptors in various animal tissues motivates the use of this …
Molecular basis of ligand selectivity for melatonin receptors
Sleep disorders in adults are related to adverse health effects such as reduced quality of life
and increased mortality. About 30–40% of adults are suffering from different sleep disorders …
and increased mortality. About 30–40% of adults are suffering from different sleep disorders …
In search of novel and therapeutically significant melatoninergic ligands
SM Mody, Y Hu, MKC Ho… - Recent Patents on CNS …, 2007 - ingentaconnect.com
Melatonin, the pineal gland hormone, is widely distributed in mammalian tissues and exerts
its action via two melatonin receptor sub-types, MT1 and MT2. Melatonin is known to play …
its action via two melatonin receptor sub-types, MT1 and MT2. Melatonin is known to play …
Synthesis and pharmacological evaluation of pentacyclic 6a, 7-dihydrodiindole and 2, 3-dihydrodiindole derivatives as novel melatoninergic ligands
MI Attia, PA Witt-Enderby, J Julius - Bioorganic & medicinal chemistry, 2008 - Elsevier
The synthesis of novel melatonin analogues 3a and 4a–c designed as melatonin receptor
ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1 …
ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1 …
Molecular modeling of human MT2 melatonin receptor: the role of Val204, Leu272 and Tyr298 in ligand binding
P Mazna, V Obsilova, I Jelinkova, A Balik… - Journal of …, 2004 - Wiley Online Library
A model of the helical part of the human MT2 melatonin (hMT2) receptor, a member of the G
protein‐coupled receptors superfamily has been generated, based on the structure of …
protein‐coupled receptors superfamily has been generated, based on the structure of …
Synthesis of novel МТ3 receptor ligands via an unusual Knoevenagel condensation
MS Volkova, KC Jensen, NA Lozinskaya… - Bioorganic & medicinal …, 2012 - Elsevier
New 5-acetamido-substituted melatonin derivatives were efficiently synthesized in excellent
yields via Knoevenagel condensation. The relative binding affinity of new synthesized …
yields via Knoevenagel condensation. The relative binding affinity of new synthesized …
Update on melatonin receptors: IUPHAR Review 20
R Jockers, P Delagrange… - British journal of …, 2016 - Wiley Online Library
Melatonin receptors are seven transmembrane‐spanning proteins belonging to the GPCR
superfamily. In mammals, two melatonin receptor subtypes exist‐MT1 and MT2‐encoded by …
superfamily. In mammals, two melatonin receptor subtypes exist‐MT1 and MT2‐encoded by …