Results 181 to 190 of about 5,798 (220)

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
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Reduced hippocampal MT₂ melatonin receptor expression in Alzheimer's disease

Journal of Pineal Research, 2004
Abstract:  The aim of the present study was to identify the distribution of the second melatonin receptor (MT2) in the human hippocampus of elderly controls and Alzheimer's disease (AD) patients. This is the first report of immunohistochemical MT2 localization in the human hippocampus both in control and AD cases.
Savaskan, Egemen, Ayoub, Mohammed A., Ravid, Rivka, Angeloni, Debora, Fraschini, Franco, Meier, Fides, Eckert, Anne, Müller-Spahn, Franz, Jockers, Ralf   +8 more
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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
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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
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A new melatonin receptor ligand with mt1‐agonist and MT2‐antagonist properties

Journal of Pineal Research, 2000
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 and pharmacological characterization of a new compound N‐{2‐[5‐(2‐hydroxyethoxy)‐1H‐indol‐3‐yl)] ethyl} acetamide or 5‐hydroxyethoxy‐N‐acetyltryptamine (5‐HEAT).
NONNO R, LUCINI V, SPADONI, GILBERTO, PANNACCI M, CROCE A, ESPOSTI D, BALSAMINI, CESARINO, TARZIA, GIORGIO, FRASCHINI F, STANKOV BM   +9 more
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4‐Substituted Anilides as Selective Melatonin MT₂ Receptor Agonists.

ChemInform, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
James R, Epperson, Jeffrey A, Deskus, Anthony J, Gentile, Lawrence G, Iben, Elaine, Ryan, Nathan S, Sarbin   +5 more
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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
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Molecular cloning and pharmacological characterization of rat melatonin MT1 and MT2 receptors

Biochemical Pharmacology, 2008
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 rMT(1) receptor was cloned using DNA fragments for exon 1 and 2 amplified from rat genomic DNA followed by screening of a rat genomic library for the full length exon ...
Valérie, Audinot, Anne, Bonnaud, Line, Grandcolas, Marianne, Rodriguez, Nadine, Nagel, Jean-Pierre, Galizzi, Ales, Balik, Sophie, Messager, David G, Hazlerigg, Perry, Barrett, Philippe, Delagrange, Jean A, Boutin   +11 more
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Molecular Modeling of Human MT1 and MT2 Melatonin Receptors

2006
Malfunction of G-protein coupled receptors (GPCR) provokes large amount of diseases. Their adequate treatment requires rational design of new high affinity and high selectivity drugs targeting these receptors. Molecular modeling represents a powerful tool to solve the problem.
A. Chugunov, P. Chavatte, R. Efremov
openaire   +1 more source

Molecular pharmacology of the mouse melatonin receptors MT1 and MT2

European Journal of Pharmacology, 2012
The main melatonin receptors are two G-protein coupled receptors named MT(1) and MT(2). Having described the molecular pharmacology of the human versions of these receptors, we turned to two of the three species most useful in studying melatonin physiology: rat and sheep (a diurnal species used to understand the relationship between circadian rhythm ...
Devavry, Séverine, Legros, Celine, Brasseur, Chantal, Cohen, William, Guénin, Sophie-Pénélope, Delagrange, Philippe, Malpaux, Benoit, Ouvry, Christine, Cogé, Francis, Nosjean, Olivier, Boutin, Jany   +10 more
openaire   +2 more sources