Results 181 to 190 of about 13,446 (217)

Molecular pharmacology of the ovine melatonin receptor: comparison with recombinant human MT1 and MT2 receptors

Biochemical Pharmacology, 2004
The variations of the pharmacological properties of melatonin receptors between different mammalian species in transfected cell lines have been poorly investigated. In the present study, melatonin analogues have been used to characterize the pharmacology of the recombinant ovine melatonin receptor (oMT1) expressed in CHO cell lines and the native oMT1 ...
Mailliet, F., Audinot, V., Malpaux, Benoit, Bonnaud, Anthony, Delagrange, P., Migaud, Martine, Barrett, P., Viaud-Massuard, M.C., Lesieur, D., Lefoulon, F., Renard, P., Boutin, Jany   +11 more
openaire   +2 more sources

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
openaire   +3 more sources

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
openaire   +4 more sources

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
openaire   +2 more sources

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

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

Functional MT1 and MT2 melatonin receptors in mammals.

Endocrine, 2005
Melatonin, dubbed the hormone of darkness, is known to regulate a wide variety of physiological processes in mammals. This review describes well-defined functional responses mediated through activation of high-affinity MT1 and MT2 G protein-coupled receptors viewed as potential targets for drug discovery.
Margarita L, Dubocovich, Magdalena, Markowska   +1 more
openaire   +1 more source

Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist

Neuropharmacology, 2005
Ramelteon (TAK-375) is a novel melatonin receptor agonist currently under investigation for the treatment of insomnia. This study describes the neurochemical and receptor binding characteristics of ramelteon in vitro. Ramelteon showed very high affinity for human MT1 (Mel1a) and MT2 (Mel1b) receptors (expressed in Chinese hamster ovary [CHO] cells ...
Koki, Kato, Keisuke, Hirai, Keiji, Nishiyama, Osamu, Uchikawa, Kohji, Fukatsu, Shigenori, Ohkawa, Yuji, Kawamata, Shuji, Hinuma, Masaomi, Miyamoto   +8 more
openaire   +2 more sources

Targeting Melatonin MT2 Receptors: A Novel Pharmacological Avenue for Inflammatory and Neuropathic Pain

Current Medicinal Chemistry, 2018
Melatonin (MLT) has been implicated in several pathophysiological states, including pain. MLT mostly activates two G-protein coupled receptors, MT1 and MT2. In this review, we present the analgesic properties of MLT in preclinical and clinical studies, giving particular emphasis to the effects mediated by MT2 receptors and to recent investigations ...
Posa, Luca, De Gregorio, Danilo, Gobbi, Gabriella, COMAI, STEFANO   +3 more
openaire   +2 more sources

Melatonin, non-selective MT1/MT2 and selective MT2 receptor agonists: differential effects on the 24-hr vigilance states

2014
Melatonin (MLT) is a neurohormone implicated in several physiological processes such as sleep. Contrasting results have been produced on whether or not it may act as a hypnotic agent, and the neurobiological mechanism through which it controls the vigilance states has not yet been elucidated.
Ochoa Sanchez, R., Comai, S., SPADONI, GILBERTO, BEDINI, ANNALIDA, TARZIA, GIORGIO, Gobbi, G.   +5 more
openaire   +1 more source