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Receptors, Melatonin (2):
Recent article
Receptors, Melatonin
Abstract
We evaluate the expression and activation of rat diaphragm or cultured skeletal muscle G-proteins using [(35)S]GTPγS. Total membrane Gα subunit content was 4-7 times higher in rat primary cultured myotubes and L6 cell line than in diaphragm (32.6±1.2fmol/mg protein) and 7-27% of them were in the...
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PMID: 21084061
PDF is available here.
PDF is available here.
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Abstract
Abstract
IMPORTANCE OF THE FIELD: Melatonin is a major chronobiological regulator involved in circadian phasing, sleep, and numerous other functions including cyto-/neuroprotection, immune modulation, and energy metabolism. The suitability of melatonin as a drug is limited because of its short half-life. The...
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PMID: 20408738
PDF is available here.
PDF is available here.
Abstract
A clean, efficient, and diasteroselective (dr >95%) catalytic hydrogenation of the enamide N-(4-phenyl-3,4-dihydronaphthalen-2-yl)propionamide (2 a) using palladium on carbon is performed. This procedure provides the melatonin receptor ligand (+/-)-cis-4-phenyl-2-propionamidotetralin...
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PMID: 20108301
PDF is available here.
PDF is available here.
Abstract
A clean, efficient, and diasteroselective (dr >95%) catalytic hydrogenation of the enamide N-(4-phenyl-3,4-dihydronaphthalen-2-yl)propionamide (2 a) using palladium on carbon is performed. This procedure provides the melatonin receptor ligand (+/-)-cis-4-phenyl-2-propionamidotetralin...
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PMID: 20108301
PDF is available here.
PDF is available here.
BMC Neuroscience (11) 2010
Abstract
These results suggest a potential synergy between melatonergic and serotonergic pathways in the action of agomelatine....
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PMID: 20525261
PDF is available here.
PDF is available here.
Lakartidningen (107)45 2010
Abstract
Abstract
The circadian production of melatonin by the pineal gland during the night provides an inhibitory signal to tissue-isolated steroid receptor SR+ and - MCF-7 human breast cancer xenografts in female nude rats. A pivotal mechanism for melatonin's anticancer effects in vivo involves a m...
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PMID: 20042410
PDF is available here.
PDF is available here.
Prescrire international (18)104 2009
Abstract
(1) When an antidepressant is considered a necessary addition to psychological support in treating patients with depression, the first-line drug is a tricyclic such as clomipramine or a selective serotonin reuptake inhibitor (SSRI) such as paroxetine; (2) Agomelatine, a melatonin receptor agonist, i...
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PMID: 20020562
PDF is available here.
PDF is available here.
Journal of Physiology and Pharmacology (60 Suppl 7) 2009
Abstract
We conclude that 1) exogenous melatonin and that released from the L-tryptophan attenuate lesions induced by topical irritant such as ethanol and WRS via interaction with MT(2) receptors and due to an enhancement of gastric microcirculation, probably mediated by NO and PG derived from cNOS, iNOS and...
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PMID: 20388945
PDF is available here.
PDF is available here.
Abstract
A variety of drugs targeting several pathways, including GABA(A) agonism, MT1/MT2 agonism, 5-HT(2A) antagonism, OX1/OX2 antagonism and others, are in Phase II and III trials. More work should be done to understand the impact of these drugs in certain populations and in the context of comorbid condit...
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PMID: 19708818
PDF is available here.
PDF is available here.
Neuropsychopharmacology (34)9 2009
Abstract
These results indicate that melatonin through its receptor can modulate the survival of newborn neurons in the adult hippocampus, making it the first known exogenously applicable substance with such specificity....
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PMID: 19421166
PDF is available here.
PDF is available here.
Prescrire international (18)101 2009
Abstract
The European Committee for Medicinal Products for Human Use (CHMP) has issued a negative opinion on the use of the melatonin receptor agonist ramelteon in insomnia, due to its unfavourable risk-benefit balance. In France, melatonin itself is licensed for use in this indication.
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PMID: 19639675
PDF is available here.
PDF is available here.
Abstract
Ramelteon 8 mg, on average, reduced LPS by approximately 13 min more than placebo on nights 1 and 2 of treatment in adults with chronic insomnia. Ramelteon was well tolerated with a low incidence of adverse events. This mean reduction in LPS versus placebo is similar to what has been reported for ot...
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PMID: 19327100
PDF is available here.
PDF is available here.
Hypertension Research (32)4 2009
Abstract
Our results suggest that L-NAME treatment enhances melatonin production in the pineal gland, potentially by decreasing an inhibitory effect of NO on melatonin production in the pineal gland. However, the enhanced pineal melatonin formation was insufficient to increase melatonin concentrations in cir...
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PMID: 19262491
PDF is available here.
PDF is available here.
Abstract
Melatonin influences the second messenger cyclic guanosine 3',5'-monophosphate (cGMP) signaling pathway in pancreatic beta-cells via a receptor-mediated mechanism. In the present study, it was determined how the regulation of cGMP concentrations by melatonin proceeds. The results provide evidence th...
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PMID: 19175857
PDF is available here.
PDF is available here.
Abstract
A novel series of 2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues has been prepared to probe the steric and electronic properties of the binding pocket of the MT(2) receptor accommodating the "out-of-plane" substituent of MT(2)-selective antagonists. The acetamide (6b) beari...
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PMID: 19193160
PDF is available here.
PDF is available here.
Abstract
We also highlighted a role of cAMP in the pathway, because forskolin mimicked the effects of luzindole and/or PGE(2) in the RORalpha expression. Finally, a significant RORalpha downregulation was observed in T cells permanently transfected with inducible MT(1) antisense. In conclusion, we show a nov...
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PMID: 19099187
PDF is available here.
PDF is available here.
Abstract
Animal Reproduction Science (110)1-2 2009
Abstract
The reproductive activity of goats bred in temperate latitude follows a seasonal pattern, influenced by annual variation in day length. Daily variation in pineal melatonin secretion is the neuroendocrine signal recognized by animals through the link between this hormone and melatonin receptor 1a (MT...
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PMID: 18243602
PDF is available here.
PDF is available here.
Nature Genetics (41)1 2009
Abstract
We show that the risk genotype of this SNP predicts future type 2 diabetes (T2D) in two large prospective studies. Specifically, the risk genotype was associated with impairment of early insulin response to both oral and intravenous glucose and with faster deterioration of insulin secretion over tim...
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PMID: 19060908
PDF is available here.
PDF is available here.
Molecular Vision (15) 2009
Abstract
Mel1a, Mel1b, and Mel1c receptor subtypes are expressed in the lateral plasma membrane of the Xenopus surface CE, at a position in close proximity to the tight junctions that form the corneal diffusion barrier. The very close association of the Mel1a receptors to the ZO-1 peripheral membrane tight j...
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PMID: 19936310
PDF is available here.
PDF is available here.
Nature Genetics (41)1 2009
Abstract
We identified rs1387153, near MTNR1B (which encodes the melatonin receptor 2 (MT2)), as a modulator of fasting plasma glucose (FPG; P = 1.3 x 10(-7)). In European populations, the rs1387153 T allele is associated with increased FPG (beta = 0.06 mmol/l, P = 7.6 x 10(-29), N = 16,094), type 2 diabetes...
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PMID: 19060909
PDF is available here.
PDF is available here.
Nature Genetics (41)1 2009
Abstract
We examined the leading association signals in ten genome-wide association scans involving a total of 36,610 individuals of European descent. Variants in the gene encoding melatonin receptor 1B (MTNR1B) were consistently associated with fasting glucose across all ten studies. The strongest signal wa...
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PMID: 19060907
PDF is available here.
PDF is available here.
Abstract
The obtained data and our previous studies conducted on Colon 38 cancer indicate that membrane melatonin receptors are not indispensable to the oncostatic action of melatonin and thus other pathways such as nuclear signaling and receptor-independent mechanism may be also involved....
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PMID: 20035258
PDF is available here.
PDF is available here.
Abstract
The interaction of afobazole (5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole dihydrochloride) and its main metabolite M-11 (2-[2-(3-oxomorpholine-4-yl)-ethylthio]-5-ethoxy benzimidazole hydrochloride) with neuroreceptors was studied using the method of radioligand analysis. The binding of afobaz...
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PMID: 19334502
PDF is available here.
PDF is available here.
Annals of Pharmacotherapy (42)12 2008
Abstract
Overall, agomelatine is a promising and well-tolerated medication for the treatment of major depressive disorder. More large-scale controlled trials are needed to gain a better understanding of the relative efficacy and safety of agomelatine....
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PMID: 19033480
PDF is available here.
PDF is available here.
Abstract
We investigated whether clock genes (Per1 and Bmal1) and the albumin D-binding protein gene (Dbp) are expressed in the EC of Syrian hamsters, and whether their expression differs under long-day and short-day conditions. Expression of all three genes followed a diurnal rhythm; expression of Per1 and...
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PMID: 19087172
PDF is available here.
PDF is available here.
Abstract
It is well-documented that melatonin influences insulin secretion. The effects are mediated by specific, high-affinity, pertussis-toxin-sensitive, G protein-coupled membrane receptors (MT(1) as well MT(2)), which are present in both the pancreatic tissue and islets of rats and humans, as well as in...
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PMID: 18624957
PDF is available here.
PDF is available here.
Abstract
The pineal hormone melatonin is able to shift the timing of circadian rhythms, including the sleep-wake cycle, and to promote sleep. Melatonin agonists with similar properties have therapeutic potential for the treatment of circadian rhythm sleep disorders. Depression is specifically targeted by ago...
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PMID: 18827285
PDF is available here.
PDF is available here.
Critical Care Medicine (36)10 2008
Abstract
Ramelteon therapy improves liver function, hepatic perfusion, and hepatocellular integrity after hemorrhagic shock in rat. This demonstrates that an isolated activation of melatonin receptors may be sufficient for organ protection, independent from direct antioxidant effects. The hypnotic ramelteon...
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PMID: 18766086
PDF is available here.
PDF is available here.
Prescrire international (17)97 2008
Abstract
(1) Patients complaining of insomnia should first be treated with non-drug measures (information, advice). Short-course benzodiazepine therapy can be tried if non-drug measures and established herbal remedies fail; (2) Ramelteon, a drug that antagonises receptors for melatonin, a hormone involved in...
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PMID: 19534018
PDF is available here.
PDF is available here.
Abstract
Melatonin, acting through its receptors, is involved in numerous physiological processes, including blood pressure (BP) regulation. In present study, the effect of melatonin inhibition on stress-induced hypertension was investigated. The hypertensive model consisted of male Sprague-Dawley rats subje...
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PMID: 18637016
PDF is available here.
PDF is available here.
Abstract
We propose that melatonin may act as a signaling molecule regulating some differentiation processes (e.g., cell proliferation, migration, etc.) before the formation of neural and hormonal systems....
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PMID: 18288645
PDF is available here.
PDF is available here.
Abstract
Six hours after WRS, there were 360 bp positive bands in RT-PCR product of MT1. The relative content of MR was lower in the model group than that in the normal group. MR content in PNS group and ranitidine group were both higher than that in the normal group and the model group (P < 0.05 or P < 0.01...
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PMID: 19112897
PDF is available here.
PDF is available here.
Abstract
We previously showed that melatonin receptors are expressed and are functional in JEG-3 and BeWo cell lines, both in vitro models of human trophoblast. Local synthesis of melatonin in placenta has been proposed, but the human placenta's ability to synthesize melatonin de novo has never been studied....
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PMID: 18312298
PDF is available here.
PDF is available here.
Abstract
Melatonin is a neurohormone that has been claimed to be involved in a wide range of physiological functions. Nevertheless, for most of its effects, the mechanism of action is not really known. In mammals, two melatonin receptors, MT1 and MT2, have been cloned. They belong to the G-protein-coupled re...
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PMID: 18493248
PDF is available here.
PDF is available here.
Pathologie Biologie (56)5 2008
Abstract
It has been confirmed that clock genes, as well as the pineal hormone, have a role in the hypothalamic suprachiasmatic nucleus, the circadian endogenous pacemaker. It seems that the peripheral clock genes in the cells of the immune system subtly control biorhythms; their seeming lack of impact only...
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PMID: 18289800
PDF is available here.
PDF is available here.
Abstract
The influences of serotonin (5-hydroxytryptamine) on the action of melatonin (N-acetyl-5-methoxytryptamine) in MIH (maturation inducing hormone)-induced meiotic resumption were evaluated in the oocytes of carp Catla catla using an in vitro model. Oocytes from gravid female carp were isolated and inc...
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PMID: 18455941
PDF is available here.
PDF is available here.
Progress in Neurobiology (85)3 2008
Abstract
We review the current knowledge about the properties and signaling of melatonin receptors as well as their potential role in health and some diseases. Melatonin MT1 and MT2 receptors are G protein coupled receptors which are expressed in various parts of the CNS (suprachiasmatic nuclei, hippocampus,...
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PMID: 18571301
PDF is available here.
PDF is available here.
Abstract
Periventricular leukomalacia is a major cause of cerebral palsy. Perinatal white matter lesions associated with cerebral palsy appears to involve glutamate excitotoxicity. When injected intracerebrally into newborn mice, the glutamatergic analog, ibotenate, induces white matter cysts mimicking human...
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PMID: 18466899
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (283)24 2008
Abstract
We show that MUPP1 binds to the G protein-coupled MT(1) melatonin receptor and directly regulates its G(i)-dependent signal transduction. Structural determinants involved in this interaction are the PDZ10 domain of MUPP1 and the valine of the canonical class III PDZ domain binding motif DSV of the M...
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PMID: 18378672
PDF is available here.
PDF is available here.
Abstract
Photoperiod exerts profound influence on the physiology of mammals through the action of melatonin on the neuroendocrine system. Over the last 20 years, studies have moved away from a melatonin receptor-focused approach to understanding how photoperiod regulates neuroendocrine activity through studi...
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PMID: 18601705
PDF is available here.
PDF is available here.
Abstract
PURPOSE: The diagnostic criteria and treatment of insomnia are reviewed. SUMMARY: Insomnia is most often described as a subjective complaint of poor sleep quality or quantity despite adequate time for sleep, resulting in daytime fatigue, irritability, and decreased concentration. Insomnia is classif...
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PMID: 18463341
PDF is available here.
PDF is available here.
Abstract
Benzofuranic analogues of MCA-NAT (5-methoxycarbonylamino-N-acetyltryptamine) have been synthesized and evaluated as melatonin receptor ligands. Introduction of a methoxycarbonylamino substituent in the C-5 position of the benzofurane nucleus obtains MT(3) selective ligands. This selectivity can be...
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PMID: 18372181
PDF is available here.
PDF is available here.
Abstract
Melatonin is known to inhibit insulin secretion from rodent beta-cells through interactions with cell-surface MT1 and/or MT2 receptors, but the function of this hormone in human islets of Langerhans is not known. In the current study, melatonin receptor expression by human islets was examined by rev...
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PMID: 18194202
PDF is available here.
PDF is available here.
Brain Research (1200) 2008
Abstract
We report that both mechanical allodynia and depression-like behavior were significantly exacerbated after peripheral nerve injury in Wistar-Kyoto (WKY) rats, a genetic variation of Wistar rats with demonstrable depression-like behavior. Administration of melatonin into the anterior cingular cortex...
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PMID: 18289511
PDF is available here.
PDF is available here.
Abstract
Many biological processes display circadian rhythms in activity, which presumably operate to coordinate cellular functions with daily environmental oscillations. The diurnal changes in environmental illumination are conveyed by the retina to the brain to entrain circadian rhythms throughout the body...
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PMID: 18316227
PDF is available here.
PDF is available here.
Abstract
We investigated the day/night differences in melatonin membrane receptor mRNA expression in chicken lymphoid organs and cultured splenocytes and examined the in vitro effect of melatonin and 2-iodomelatonin on the intracellular Ca(2+) concentration ([Ca(2+)](i)) in chicken splenocytes. In whole orga...
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PMID: 18289164
PDF is available here.
PDF is available here.
Abstract
Insomnia is the most common sleep disorder in the industrialized world. A variety of precipitating events have been identified, but when it becomes a persistent problem, maladaptive patterns become established, thereby, perpetuating the sleep disturbance. Individuals with insomnia have impaired next...
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PMID: 18220487
PDF is available here.
PDF is available here.
Abstract
We investigated the temperature-dependence of 2-iodo-melatonin ([(125)I]Mel) binding in the optic tectum-tegmentum area and the neural retina. The binding of [(125)I]Mel showed a widespread distribution in brain and ocular tissues, with the highest density in the optic tectum-thalamus and the lowest...
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PMID: 18177872
PDF is available here.
PDF is available here.
Abstract
Melatonin (N-acetyl-5-methoxytryptamine) is synthesized and released by the pineal gland following a circadian rhythm characterized by high levels during the night. It shows several pharmacological effects on diverse cellular and animal models, mainly related to either its antioxidan...
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PMID: 18673165
PDF is available here.
PDF is available here.
Critical Care Medicine (36)1 2008
Abstract
Melatonin therapy after hemorrhagic shock improves liver function, hepatic perfusion, redox state, and hepatic integrity. With respect to liver function, beneficial effects of the pineal hormone seem to be dependent on melatonin receptor activation....
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PMID: 18090374
PDF is available here.
PDF is available here.
Critical Care Medicine (36)1 2008
Abstract
Abstract
Melatonin, a ubiquitous methoxyindole, is produced by and metabolized in the skin. Melatonin affects skin functions and structures through actions mediated by cell-surface and putative-nuclear receptors expressed in skin cells. Melatonin has both receptor-dependent and receptor-independent effects t...
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PMID: 18155917
PDF is available here.
PDF is available here.
Abstract
Each year millions of travelers undertake long distance flights over one or more continents. These multiple time zone flights produce a constellation of symptoms known as jet lag. Familiar to almost every intercontinental traveler is the experience of fatigue upon arrival in a new time zone, but alm...
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PMID: 18342269
PDF is available here.
PDF is available here.
Abstract
Using an in silico approach, we demonstrated that GPR50 is the ortholog of the high affinity Mel1c receptor. It was necessary to also study the synteny of this gene to reach this conclusion because classical mathematical models that estimate orthology and build phylogenetic trees were not sufficient...
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PMID: 18400093
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (58)1 2008
Abstract
Melatonin (CAS 73-31-4) has both hypnotic and sleep/wake rhythm regulating properties. These sleep promoting actions, which are already demonstrable in healthy humans, have been found useful in subjects suffering from circadian rhythm sleep disorders (CRSD) like delayed sleep phase syndrome (DSPS),...
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PMID: 18368944
PDF is available here.
PDF is available here.
Abstract
Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for the treatment of insomnia characterized by difficulty in sleep onset. It is a nonscheduled drug since it lacks the potential for abuse and does not interact with neurotransmitter receptors most associated wit...
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PMID: 18296808
PDF is available here.
PDF is available here.