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Receptor, Melatonin, MT2 (0):
Recent article
Receptor, Melatonin, MT2
Oral Diseases (16)7 2010
Abstract
To define the influence of cholecystokinin and melatonin on the inflammatory response of the lipopolysaccharide-exposed rat parotid gland.
Bacterial lipopolysaccharide was infused retrogradely into the parotid duct. The degree of inflammation three hours postadministration was estimated from the act...
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PMID: 20846152
PDF is available here.
PDF is available here.
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Annals of Medicine (42)6 2010
Abstract
The incidence of type 2 diabetes mellitus has markedly increased worldwide over the past decades. Pancreatic beta-cell dysfunction as well as central and peripheral insulin resistance appears to be elementary features in the pathophysiology of type 2 diabetes mellitus. Major environmental conditions...
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PMID: 20597807
PDF is available here.
PDF is available here.
Abstract
We tested the hypothesis that ramelteon would reduce core temperature, increase the DPG, as well as shorten SOL, reduce wakefulness after sleep onset (WASO), and increase total sleep time (TST) during a daytime sleep opportunity....
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PMID: 20550024
PDF is available here.
PDF is available here.
Abstract
To demonstrate the clinical effectiveness of an antidepressant drug requires evidence beyond short- and long-term efficacy, including a favourable adverse-effect profile and sustained treatment adherence. Under these conditions, patients should experience enhanced social and functional outcomes. The...
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PMID: 20192279
PDF is available here.
PDF is available here.
Abstract
Agomelatine (beta-methyl-6-chloromelatonin), which is structurally homologous to melatonin, is a potent agonist of melatonin MT1 and MT2 receptors as well as an antagonist of serotonin 5-HT(2C) receptors. Agomelatine appears to improve sleep without causing daytime sedation. It has not been found to...
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PMID: 19758108
PDF is available here.
PDF is available here.
Abstract
The findings are important in 2 respects. First, agomelatine is an effective and safe antidepressant continuation therapy, which confirms efficacy seen in short-term studies. Second, few early relapses were observed in the patient group switched to placebo: the survival curve for placebo separated g...
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PMID: 19689920
PDF is available here.
PDF is available here.
Abstract
Current treatment of insomnia with hypnotics, GABA(A) receptor modulators, induces various side effects, including cognitive impairment, motor disturbance, dependence, tolerance, hang-over, and rebound insomnia. Ramelteon (Rozerem) is an orally active, highly selective melatonin MT1/MT2 receptor ago...
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PMID: 19768947
PDF is available here.
PDF is available here.
Abstract
Two novel series of melatonin-derived compounds have been synthesized and pharmacologically evaluated at the MT(1) and MT(2) subtypes of melatonin receptors. Compounds 12b-c are non-selective high-affinity MT(1) and MT(2) receptor ligands (K(i)=7-11 nM). Compound 12b had little intri...
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PMID: 19473848
PDF is available here.
PDF is available here.
Abstract
We investigated the effect of melatonin against experimental RE in rats. Melatonin pretreatment significantly reduced the haemorrhagic lesions and decreased esophageal lipid peroxidation aggravated by RE. Moreover, the depleted levels of superoxide dismutase and glutathione observed in RE were reple...
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PMID: 19067786
PDF is available here.
PDF is available here.
Abstract
We extended our findings to MT2 melatonin receptors using both in vitro and in vivo approaches. Using CHO cells expressing human MT2 melatonin receptors, microtubule depolymerization prevents the loss in the number of high potency states of the receptor when compared to melatonin-treated cells. In a...
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PMID: 19175856
PDF is available here.
PDF is available here.
Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine (5)1 2009
Abstract
Significant symptom reduction was observed on all scales (HAMA, ESS, CGI-I, CGI-S), with subjects falling asleep faster and sleeping longer. Headache upon stopping ramelteon, daytime tiredness, agitation, and depression were the most commonly reported side effects and were cited as transient. CONCLU...
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PMID: 19317378
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.
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.
The effect of melatonergic and non-melatonergic antidepressants on sleep: weighing the alternatives.
Abstract
In DSM-IV the occurrence of disturbed sleep is one of the principal diagnostic criteria for major depressive disorder (MDD). Further, there is evidence of reciprocity between the two conditions such that, even in the absence of current depressive symptoms, disturbed sleep often predicts their develo...
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PMID: 18609422
PDF is available here.
PDF is available here.
Neuroendocrinology (90)3 2009
Abstract
Melatonin has been implicated in the control of the reproductive system, and the modulatory actions of melatonin on gonadotropin-releasing hormone (GnRH) neurons have been assumed to be indirectly mediated through afferent neurons. However, our previous studies demonstrate sexually dimorphic modulat...
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PMID: 19641296
PDF is available here.
PDF is available here.
Abstract
Antidepressant pharmacotherapy forms the basis of management of major depressive disorder (MDD). In principle, the management of MDD should first elicit rapid relief of symptoms and then restore normal functioning and prevent relapse. It is recommended that treatment should continue for at least one...
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PMID: 19708725
PDF is available here.
PDF is available here.
Abstract
Currently available antidepressant agents such as tricyclic antidepressants (TCAs) act primarily through monoaminergic systems in the brain, and have proved to be suboptimal for the management of major depressive disorder (MDD). Such agents are also active at non-target receptor sites, contributing...
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PMID: 19708723
PDF is available here.
PDF is available here.
Abstract
Melatonin, the main hormone produced by the pineal gland, strongly inhibits the growth of cancer cells in vitro and in vivo. Some publications indicate that the addition of melatonin to culture medium slows the proliferation of some cancer cell lines. It is also suggested that melato...
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PMID: 19837985
PDF is available here.
PDF is available here.
Abstract
We have cloned cDNAs of two rat membrane melatonin receptor subtypes, melatonin receptor 1a (MT1) and melatonin receptor 1b (MT2), using a rapid amplification of cDNA end (RACE) method. The rat MT1 and MT2 cDNAs encode proteins of 353 and 364 amino acids, respectively, and show 78-93% identities wit...
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PMID: 19340560
PDF is available here.
PDF is available here.
Abstract
Melatonin is a mammalian hormone that has a great variety of effects. At present there is evidence that this hormone considerably reduces the manifestations of many gastrointestinal inflammatory diseases. The biological effects of melatonin are realized through the receptors located on the membranes...
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PMID: 19253695
PDF is available here.
PDF is available here.
Revista Medica de Chile (136)11 2008
Abstract
The expression of MT1 melatonin receptor in the human adrenal, and the melatonin reduction of ACTH-stimulated cortisol production suggest a direct melatonin action on the adrenal gland....
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PMID: 19301769
PDF is available here.
PDF is available here.
Abstract
We found that the increased cAMP levels induced by melatonin can be corrected by the treatment of the cells with 17-beta-estradiol. Thus, estrogens or estrogen receptor agonists become important compounds to consider in AIS osteoblast cell functioning. Consequently, our results add a new facet to th...
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PMID: 18507714
PDF is available here.
PDF is available here.
Abstract
This study suggests that agomelatine is effective in the treatment of GAD and is well tolerated. Additional trials, using an active comparator and extending over a longer period, are needed to delineate the place of agomelatine in the contemporary pharmacotherapy for anxiety disorders....
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PMID: 18794654
PDF is available here.
PDF is available here.
Abstract
We have reported the induction of glial cell line-derived neurotrophic factor, a potent survival factor for dopaminergic neurons, in the C17.2 neural stem cell line following in vitro treatment with melatonin. Furthermore, we have detected the melatonin MT(1) receptor in these cells. Given these fin...
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PMID: 18373554
PDF is available here.
PDF is available here.
Abstract
A series of naphthalenic analogues of melatonin were prepared and evaluated as melatonin receptor MT(2) selective ligands. Activity and MT(2) selectivity can be modulated with suitable variations of the C-3 phenyl and the acyl group on the C-1 side chain. Surprisingly, in contrast with what had been...
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PMID: 18778943
PDF is available here.
PDF is available here.
Neuroscience (155)4 2008
Abstract
We characterized its action on neuronal ERK1/2. We used CGC cultures prepared from the cerebella of wild-type mice (MT1/MT2 CGC) and MT1- and MT2-knockout (KO) mice (MT1 KO CGC and MT2 KO CGC, respectively), and we employed a Western blot assay to evaluate ERK1/2 phosphorylation. Ramelteon increased...
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PMID: 18664376
PDF is available here.
PDF is available here.
European Psychiatry (23)6 2008
Abstract
The clinical finding that depressive disorders are often associated with desynchronization of internal rhythms has encouraged the idea that resetting normal circadian rhythms may have antidepressant potential. Agomelatine, a naphthalene analog of melatonin, is both an agonist of human cloned melaton...
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PMID: 18583104
PDF is available here.
PDF is available here.
Journal of Psychopharmacology (22)7 Suppl 2008
Abstract
We would hope. Agomelatine is a new antidepressant with a novel profile of pharmacological action. Its efficacy in major depression has been reported in short-term placebo-controlled trials and in direct head-to-head comparison with existing products. The pooling of data from the agomelatine short-t...
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PMID: 18753277
PDF is available here.
PDF is available here.
Journal of Psychopharmacology (22)7 Suppl 2008
Abstract
Most of the available antidepressants, with different pharmacological profiles, such as inhibitors of serotonin reuptake (SSRIs) or norepinephrine reuptake (NRIs) or both (SNRIs), have limitations leading some patients to drop out of treatment. Another direction of research has therefore been undert...
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PMID: 18753276
PDF is available here.
PDF is available here.
Journal of Psychopharmacology (22)7 Suppl 2008
Abstract
Major depressive disorder (MDD) is a prevalent condition with substantial heterogeneity in terms of clinical symptom profiles, overlapping syndromes and degree of severity. The challenge for any new antidepressant is to demonstrate efficacy across the spectrum of patient subpopulations with a diagno...
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PMID: 18753279
PDF is available here.
PDF is available here.
Journal of Psychopharmacology (22)7 Suppl 2008
Abstract
Desynchronisation of normal circadian rhythms, including the sleep-wake rhythm, is common in major depressive disorder (MDD). The association between sleep disturbances and depression has long been recognised. Disturbed sleep is a diagnostic criterion for MDD, and insomnia commonly precedes the onse...
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PMID: 18753278
PDF is available here.
PDF is available here.
Journal of Psychopharmacology (22)7 Suppl 2008
Abstract
Abstract
Melatonin is a phylogenetically well-preserved molecule with diverse physiological functions. In addition to its well-known regulatory control of the sleep/wake cycle, as well as circadian rhythms generally, melatonin is involved in immunomodulation, hematopoiesis, and antioxidative processes. Recen...
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PMID: 18815150
PDF is available here.
PDF is available here.
Abstract
We examined whether melatonin, a potent anti-oxidant and free radical scavenger, would attenuate apoptotic death of rat C6 astroglial cells under glutamate excitotoxicity and oxidative stress. Exposure of C6 cells to 500 microM L-glutamic acid (LGA) and 100 microm hydrogen peroxide (H(2)O(2)) for 24...
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PMID: 18373557
PDF is available here.
PDF is available here.
Abstract
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-ylmethyl)-melatonin 4b displayed the highest affinity for MT(1) receptors (K(i)=9.8 nM) and for MT(2) subtype (K(i)=7.8 nM)...
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PMID: 18657980
PDF is available here.
PDF is available here.
Sleep Medicine Reviews (12)4 2008
Abstract
Ramelteon is a novel hypnotic compound that is FDA-approved for the treatment of sleep-onset difficulty. It is a melatonin 1/2 receptor agonist with rapid absorption, extensive first-pass metabolism and an elimination half-life of just over 1h. Clinical efficacy data indicate moderate efficacy in re...
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PMID: 18603221
PDF is available here.
PDF is available here.
Abstract
We investigated the effect of 2 wk continuous postinfarction subcutaneous melatonin supply on the expression of the rat left ventricular (LV) dihydropyridine receptor (DHPR), ryanodine receptor (RyR(2)), and sarco-endoplasmic reticulum Ca(2+)-ATPase2 (SERCA2), as they are fundamental proteins in car...
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PMID: 18284551
PDF is available here.
PDF is available here.
Clinical Therapeutics (30)7 2008
Abstract
In this post hoc analysis of data from patients with chronic insomnia, a significantly greater percentage experienced a > or = 50% reduction in LPS with ramelteon 8 mg/d versus placebo. This improvement was evident at week 1 and was sustained through 5 weeks of treatment. Ramelteon 8 mg was well tol...
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PMID: 18691991
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.
Neuroscience Letters (439)1 2008
Abstract
We used a clinically available novel agonist for MT1 and MT2 melatonin receptors, ramelteon. Primary cultures of cerebellar granule cells (CGC) have been established as an in vitro model for studying neuronal BDNF. We took advantage of the availability of MT1- and MT2-deficient (knockout; KO) mice t...
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PMID: 18501512
PDF is available here.
PDF is available here.
Abstract
We studied the role of MT in regulating the viability and differentiation of NSCs derived from rat ventral midbrain. (2) NSCs were isolated from the rat ventral midbrain. The viability of NSCs was determined by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-ulfophenyl)-2H-tetrazolium a...
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PMID: 17912627
PDF is available here.
PDF is available here.
Biochemical Pharmacology (75)10 2008
Abstract
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 sequences. Th...
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PMID: 18384758
PDF is available here.
PDF is available here.
Abstract
We have recently shown that melatonin antagonizes damage-induced apoptosis by interaction with the MT-1/MT-2 plasma membrane receptors. Here, we show that melatonin interferes with the intrinsic pathway of apoptosis at the mitochondrial level. In response to an apoptogenic stimulus, melatonin allows...
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PMID: 18339127
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.
Endocrinology (149)3 2008
Abstract
We previously demonstrated that melatonin is involved in the regulation of adrenal glucocorticoid production in diurnal primates through activation of MT1 membrane-bound melatonin receptors. However, whether melatonin has a similar role in nocturnal rodents remains unclear. Using an integrative appr...
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PMID: 18039783
PDF is available here.
PDF is available here.
Abstract
A novel, efficient and diastereoselective procedure was developed for the gram-scale synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT), a selective MT(2) melatonin receptor antagonist. The synthetic strategy involved the conversion of 4-phenyl-2-tetralone to enamide followed by diastereose...
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PMID: 18075659
PDF is available here.
PDF is available here.
Abstract
Ramelteon (Rozerem) is the first melatonin receptor agonist to be approved for the treatment of insomnia; it is not classified as a controlled substance. In patients with chronic insomnia, objectively assessed latency to persistent sleep (LPS) at week 1 was improved with oral ramelteon 8 mg administ...
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PMID: 18729542
PDF is available here.
PDF is available here.
Folia medica Cracoviensia (49)3-4 2008
Abstract
Melatonin (MT) plays an important role in the regulation of physiological and neuroendocrine functions, such as control of circadian rhythms and synchronization of seasonal reproductive rhythms in mammals. Melatonin shows its antinocieeptive effects in a dose - dependent manner. Melatonin is influen...
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PMID: 20050582
PDF is available here.
PDF is available here.
Abstract
During vertebrate neurodevelopment, neuritogenesis and synaptogenesis are modulated by intracellular cAMP rises. Melatonin, which is implicated in neuronal differentiation, mainly inhibits this pathway. Here, an investigation about the profile of this effect during the vertebrate neurodevelopment is...
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PMID: 18343081
PDF is available here.
PDF is available here.
Abstract
A novel series of melatonin receptor ligands, characterized by a N-(substituted-anilinoethyl)amido scaffold, along with preliminary structure-activity relationships (SARs), is presented. MT1 and MT2 receptor binding affinity and intrinsic activity have been modulated by the introduction of different...
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PMID: 18052314
PDF is available here.
PDF is available here.
European Journal of Pharmacology (577)1-3 2007
Abstract
The purpose of this study was to assess the antinociceptive and antiallodynic effect of melatonin as well as its possible mechanism of action in diabetic rats. Streptozotocin (50 mg/kg) injection caused hyperglycemia within 1 week. Formalin-evoked flinching was increased in diabetic rats as compared...
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PMID: 17920585
PDF is available here.
PDF is available here.
Abstract
The antiallodynic effect of melatonin after intrathecal (it) and oral administration as well as the possible participation of MT(2) and opioid receptors in melatonin-induced antiallodynia in neuropathic rats were assessed. Ligation of the L5/L6 spinal nerves produced a clear-cut tactile allodynia in...
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PMID: 17346886
PDF is available here.
PDF is available here.
Abstract
Racemic N-(8-methoxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ylmethyl)acetamide (compound 5) was previously identified as a novel selective MT(2) antagonist fulfilling the requirements of pharmacophore and 3D QSAR models. In this study the enantiomers of 5 were separated by medium-pressure liqui...
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PMID: 17907131
PDF is available here.
PDF is available here.
Abstract
The circadian release of the hormone melatonin is regulated by the suprachiasmatic nucleus (SCN), which feeds back into the nucleus to modulate sleep and circadian phase through activation of the MT(1) and/or MT(2) melatonin receptors. Considering the functions of the SCN as a sleep and circadian rhy...
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PMID: 18032103
PDF is available here.
PDF is available here.
Neuroreport (18)16 2007
Abstract
We demonstrate for the first time that glycine-induced currents from a population of isolated ganglion cells in the rat retina are potentiated by melatonin of nanomolar concentrations by increasing the efficacy and the channel conductance of the strychnine-sensitive glycine receptor. The melatonin e...
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PMID: 17921866
PDF is available here.
PDF is available here.
International Clinical Psychopharmacology (22 Suppl 2) 2007
Abstract
Full remission of symptoms is the goal for the acute treatment of depression, because incomplete remission is associated with poor outcomes including higher risk of relapse and chronicity. The current definitions for remission (e.g. a score of
PDF is available here.
PDF is available here.
Cell and Tissue Research (330)1 2007
Abstract
We have performed immunocytochemical analyses for PER1, CRY2, and pCREB in retinae of melatonin-proficient wild type (WT) mice and mice with targeted deletions of the MT1 receptor (MelaaBB) or the MT1 and MT2 receptors (Melaabb) at four different time points. Immunoreactions for PER1, CRY2 and pCREB...
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PMID: 17701055
PDF is available here.
PDF is available here.
International Clinical Psychopharmacology (22 Suppl 2) 2007
Abstract
Depressive disorders are of the highest socioeconomic and health-economic importance, as they are the psychiatric disorders that most frequently cause psychosocial disability. Despite the progress that has been made, currently available pharmacotherapies for depression still have a limited antidepre...
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PMID: 17917562
PDF is available here.
PDF is available here.
International Clinical Psychopharmacology (22 Suppl 2) 2007
Abstract
Sleep disturbances are often associated with depression and mood disorders, and certain manipulations of the sleep-wake cycle are effective as therapeutic interventions in the treatment of depression. Dysregulated circadian rhythms are thereby considered as causal. Circadian rhythms in mammals are m...
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PMID: 17917564
PDF is available here.
PDF is available here.