Abstract
We provide a comprehensive search through several key patent collections. We have covered promising small molecule compounds which are being evaluated in different clinical trials as well as drugs currently available in the pharmaceutical market. In addition, readers will gain a deep insight into th...
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PMID: 20716023
PDF is available here.
Abstract
Serotonin is an important neuromodulator associated with a wide range of physiological effects in the central nervous system. The exact mechanisms whereby serotonin influences brain development are not well understood, although studies in invertebrate and vertebrate model organisms are beginning to...
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PMID: 20561690
PDF is available here.
Abstract
This randomized, double-blind, placebo-controlled study investigated the efficacy and tolerability of the 5-HT6 receptor antagonist, SB-742457, in subjects with mild-to-moderate probable Alzheimer's disease (AD).
Participating subjects had a Mini-Mental State Examinat...
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PMID: 20043816
PDF is available here.
Abstract
We found that ciliary membrane proteins were highly mobile, but their diffusion was impeded at the base of the cilium by a diffusion barrier. Septin 2 (SEPT2), a member of the septin family of guanosine triphosphatases that form a diffusion barrier in budding yeast, localized at the base of the cili...
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PMID: 20558667
PDF is available here.
Abstract
We evaluated 5-HT6 receptor expression and associated biochemical mechanisms in the hippocampus of rats that had been trained in the Morris water maze (MWM), a spatial learning task. Training in the MWM induces a down-regulation of 5-HT6 receptor protein and mRNA receptor expression. The learning pr...
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PMID: 19737440
PDF is available here.
Abstract
We have previously shown that 5-hydroxytryptamine (5-HT) released from enterochromaffin cells activates 5-HT(3) receptors on the mucosal processes of myenteric Dogiel type II neurons to initiate the events underlying the CMMC. Our aims were to further investigate the roles of 5-HT(1A), 5-HT(3), and...
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PMID: 20413719
PDF is available here.
Tadashi Ishibashi,
Tomoko Horisawa,
Kumiko Tokuda,
Takeo Ishiyama,
Masaaki Ogasa,
Rie Tagashira,
Kenji Matsumoto,
Hiroyuki Nishikawa,
Yoko Ueda,
Satoko Toma,
Hitomi Oki,
Norihiko Tanno,
Ikutaro Saji,
Akira Ito,
Yukihiro Ohno and
Mitsutaka Nakamura
Abstract
These results demonstrate that lurasidone possesses antipsychotic activity and antidepressant- or anxiolytic-like effects with potentially reduced liability for extrapyramidal and CNS depressant side effects....
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PMID: 20404009
PDF is available here.
Abstract
We hypothesized that, as for other blood vessels, the 5-HT(1B/1D) and 5-HT(2B) receptor subtypes mediate contraction in RJV alongside the 5-HT(2A) receptor subtype. Endothelium-intact RJV rings were set up in an isolated organ bath for isometric tension recordings, and contractile concentration-effe...
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PMID: 20378714
PDF is available here.
Abstract
As soon as in the 1960's, the role of serotonin (5-Hydroxytryptamin, 5-HT) in psychiatric disorders was realized, which was further substantiated by several lines of evidence amounting to a huge body of knowledge. The indolamine 5-HT belongs to the class of monoamine transmitters and can be found in...
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PMID: 20340067
PDF is available here.
Abstract
Synthesis and biological evaluation of 1 ('angular') and 2 ('linear') cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines as novel ligands of the 5-HT(6) receptors are disclosed. The new compounds 1 and 2 are highly selective antagonists of the receptor with sub-nanomolar affinities (K...
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PMID: 20207539
PDF is available here.
Abstract
Depression is accompanied by an increase in activity in the amygdala and a decrease in the rostral anterior cingulate cortex (rACC), with the former attributed to a failure of the latter to exert its normal inhibitory influence. This failure is likely due to regression of synaptic connections betwee...
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PMID: 20307163
PDF is available here.
Abstract
Selective inhibition of 5-HT(7) receptors partly reduced CGRP release evoked by TGES. These findings suggest that 5-HT(7) receptors may play a role in the pathophysiology of migraine....
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PMID: 20236348
PDF is available here.
Abstract
These findings suggest that the descending serotonergic pathways and spinal 5-HT7 receptors play a crucial role in the antinociceptive and antihyperalgesic effects of tramadol and M1....
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PMID: 20179508
PDF is available here.
Abstract
Collectively, these findings suggest that PTHE specifically acts on the longitudinal muscle of distal colon in rats, and these stimulatory effects are likely mediated, at least, by activation of acetylcholinergic M(2) and M(3) receptors.
Copyright 2009 Elsevier Ireland Ltd. All rights reserved....
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PMID: 19963058
PDF is available here.
Abstract
We investigated the effects of genetic polymorphisms in the serotonin 1A, 2A, 2C, 3A, and 3B receptor, the serotonin transporter, and the cytochrome P450 2D6 (CYP2D6) genes on the occurrence of paroxetine discontinuation syndrome. A consecutive series of 56 Japanese patients who had a diagnosis of m...
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PMID: 20075642
PDF is available here.
Abstract
We analyzed the modulation of serotonin on the bradycardia induced in vivo by vagal electrical stimulation in alloxan-induced long-term diabetic rats. Bolus intravenous administration of serotonin had a dual effect on the bradycardia induced either by vagal stimulation or exogenous Ach, increasing i...
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PMID: 21403818
PDF is available here.
Abstract
Although the 5-HT(5) receptor subfamily was discovered more than 15 years ago, it is unambiguously the least known 5-HT receptor subtype. The G(i)/G(0)-mediated signal transduction and its intensive presence in raphe and other brainstem and pons nuclei suggest mechanisms similar to t...
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PMID: 20166946
PDF is available here.
Abstract
We describe the neuroanatomy and neurochemistry of brain serotonergic circuitries. The contribution of emergent in vivo imaging methods to the regional localization of binding site receptors and certain aspects of their functional connectivity in correlation to behavior is also discussed. 5-HT cell...
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PMID: 21319493
PDF is available here.
Abstract
We used in vivo microdialysis to examine: first, the effects of MK-801, on the efflux of glutamate and serotonin (5-HT) in the medial prefrontal cortex (mPFC) of the rat; second, whether the MK-801-induced changes in the cortical efflux of both transmitters could be blocked by atypical (clozapine an...
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PMID: 19909228
PDF is available here.
Abstract
OBJECTIVE: Following more than a century of cocaine hydrochloride extraction from Erythroxylon coca, this drug remains representing a serious social and public health problema around the world. This paper intends to provide a review about the cocaine theme, focusing on historical background and on i...
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PMID: 20470473
PDF is available here.
Abstract
These results raise the possibility that MEGL is effective against pruritus mediated by proteinases and 5-HT and that primary afferents expressing PAR(2) and 5-HT(2A) receptors are the sites of its action....
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PMID: 20460776
PDF is available here.
Abstract
The serotonin hypothesis of pulmonary arterial hypertension (PAH) arose after an outbreak of PAH in patients taking the anorexigenic drugs aminorex and dexfenfluramine. Both of these drugs are serotonin transporter (SERT) substrates and indirect serotinergic agonists. There is now a wealth of eviden...
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PMID: 20204739
PDF is available here.
Abstract
We review the role of localization and internalization as a novel mechanism for acute regulation of KV channels and pulmonary vascular tone by agonists such as serotonin....
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PMID: 20204744
PDF is available here.
Abstract
Pharmacogenetics/pharmacogenomics has been developed so rapidly in these twenty years and the pharmacogenetic/pharmacogenomic research in psychiatry is also the case. Especially, the impact of genetic polymorphism (e.g., cytochrome P450 (CYP)) on pharmacokinetics of psychotropics have been extensive...
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PMID: 20077810
PDF is available here.
Abstract
Development of anaphylactic shock initiated with the horse serum (anaphylactic index = 4.0 +/- 0.0 arbitrary units) leads to acute decrease in spleen concentration of serotonin (in shock--0.443 +/- 0.005; basal level--1.532 +/- 0.004 ng per mg of protein). Unlike of anaphylaxis, development of endot...
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PMID: 20804067
PDF is available here.
Abstract
These results demonstrate that the 5-HT1 receptors mediating sympatho-inhibition on the systemic vasculature of pithed rats resemble the pharmacological profile of the 5-HT1A, 5-HT1B, and 5-HT1D subtypes....
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PMID: 20361490
PDF is available here.
Abstract
We examined the relationship between P-5HT-R and P-PLT-A in mice by comparing the platelet count in the blood with the endogenous 5HT in the tissues (a marker for platelets because the 5HT is largely contained within platelets). 5HT levels in murine blood and tissues were also examined after intrave...
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PMID: 19967158
PDF is available here.
Abstract
We tested the hypothesis that episodic spinal 5-HT receptor activation (without AIH) is sufficient to elicit an NADPH oxidase-dependent facilitation of phrenic motor output (pMF). In anaesthetised, artificially ventilated adult male rats, episodic intrathecal 5-HT injections (3 x 6 microl injections...
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PMID: 19805745
PDF is available here.
Abstract
We review the fundamental ground work upon which this field of research was established and the work that has more recently begun to uncover the complexity of GPCR signaling. The emerging signaling paradigm includes (i) the capacity of one receptor to couple to and initiate pathways through multiple...
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PMID: 20021461
PDF is available here.
Abstract
Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT(6) serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellen...
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PMID: 19739674
PDF is available here.
Abstract
The past two decades have seen an explosion in research in the fields of violence and behavioural genetics. Advances in human genetics have raised the possibility that genetic mechanisms can explain various aspects of human criminal and aggressive behaviour. However, this new knowledge can pose enor...
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PMID: 20025103
PDF is available here.
Abstract
There are gene polymorphisms changing the expression or activation of the serotonin (5-HT) receptors, which are associated with pain. This review showed an availability of 5-HT2A receptor gene polymorphism in analgesic sensitivity. To search gene polymorphisms related to analgesic sensitivity is imp...
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PMID: 19764436
PDF is available here.
Abstract
Atypical (second generation) antipsychotic drugs have radically changed and revolutionized the pharmacological treatment of schizophrenia and related disorders. The currently approved atypical antipsychotic drugs, which are available, are characterized by relatively weak affinities for D2-type dopam...
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PMID: 19643718
PDF is available here.
Abstract
We report the long-term effect (in adolescence) of this intervention on the expression of synaptophysin, GAP-43, VGluT1, VGAT, MAP-2, spinophilin, and 5-HT1A and 5-HT2A receptors, in the anterior cingulate cortex (ACC; supragenual and subgenual areas) and amygdala (lateral, basal and central nuclei)...
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PMID: 19102816
PDF is available here.
Abstract
We discuss the role of this recently discovered G protein-coupled receptor in cognition and memory, particularly in Alzheimer's disease. A surge in publications that describe the development of ligands for this receptor have recently come to light, underscoring the emerging interest in this receptor...
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PMID: 19589055
PDF is available here.
Abstract
These results indicate that 5-HT(7a) receptor antagonism, and not D(2)/D(3) receptor antagonism, likely underlies the antidepressant actions of amisulpride....
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PMID: 19337725
PDF is available here.
Abstract
We selected positron emission tomography (PET) and single photon emission computed tomography (SPECT) studies of antipsychotic dose vs occupancy at both temporal cortex and striatal D(2)/D(3) receptors. We selected corresponding SPECT and PET studies of 5HT(2A) receptor occupancy. We also selected r...
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PMID: 18303092
PDF is available here.
Abstract
We show that some antipsychotic drugs produce significant functional changes in serotonergic neurons that directly impact feeding behavior in the model organism, Caenorhabditis elegans. In particular, antipsychotic drugs acutely suppress pharyngeal pumping, which is regulated by serotonin from the N...
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PMID: 19447297
PDF is available here.
Abstract
We performed a 40 ns molecular dynamics simulation of the mGluR2/5HT(2A) heterocomplex constructed around a TM4/TM5 interface and embedded in an explicit phospholipidic bilayer surrounded by water molecules. In a separate experiment, the monomeric 5HT(2A) receptor was simulated for additional 40 ns...
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PMID: 19422244
PDF is available here.
Abstract
Although the field still struggles with the lack of major breakthroughs, some novel pharmacological leads have provided encouraging findings in proof of concept or early phase II clinical trials. Although some of these approaches are based on the modified dopamine/glutamate hypothesis of schizophren...
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PMID: 19346948
PDF is available here.
Abstract
We examine the role of the serotonergic system in regulating locomotor behavior of decerebrated cats during ES at L4-L5. ES elicited coordinated, weight-bearing, hindlimb stepping with plantar foot placement on a moving treadmill belt. Ketanserin [a 5-hydroxytryptamine (serotonin) (5-HT)(2/7) recept...
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PMID: 19403834
PDF is available here.
Abstract
There are important differences in discriminative stimulus properties both between and within atypical and typical antipsychotics and across species. While low-dose clozapine discrimination in rats appears to provide a more sensitive behavioral assay for distinguishing atypical from typical antipsyc...
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PMID: 18795269
PDF is available here.
Abstract
We identified brain regions that exhibit 5-carboxyamidotryptamine, ritanserin, and LY344864 - insensitive [(3)H]5-HT binding (characteristic of the 5-HT(1E) receptor). In hippocampal homogenates, where 5-HT(1E) receptor density was sufficiently high for radioligand binding analysis, 100 nM 5-carboxy...
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PMID: 19200348
PDF is available here.
Abstract
These results raise significant concerns about studies using NAN-190 and SB 269970 as specific antagonists of serotonin receptors....
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PMID: 19190523
PDF is available here.
Abstract
Scaffold selection involving an indole-to-indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides...
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PMID: 19159187
PDF is available here.
Abstract
Recent literature has explored several novel concepts in the association of serotonin and symptoms, alterations in tissue levels of serotonin and its reuptake protein, aspects of the genetic determinants of serotonergic function (particularly 5-HTTLPR) and its relationship to gastrointestinal motor...
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PMID: 19115522
PDF is available here.
Abstract
Zotepine is a second generation antipsychotic drug, a substituted dibenzothiepine tricyclic molecule, with effects on dopamine, serotonin and noradrenaline receptors. This article reviews the relevant research studies on the drug based on a search of numerous medical databases for research and liter...
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PMID: 19199377
PDF is available here.
Abstract
These results suggest that goshuyuto constricts rat aorta strips and that the mechanisms involve the adrenergic and/or serotonergic receptors. Also, it may be suggested that Evodiae Fructus and synephrine play the important role in the vasoconstrictive effects of goshuyuto on rat aorta strips....
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PMID: 19182382
PDF is available here.
Abstract
Interplay between migraine and balance disorder morbidities has been a topic of interest for many years. Serotonin (5-HT) receptor is closely related with migraine and is associated with vestibular symptoms. The mechanism underlying migrainous vertigo, however, has not been determined. 5-HT1F recept...
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PMID: 19077678
PDF is available here.
Abstract
We report a high-throughput method for genotyping of single nucleotide polymorphisms (SNPs) within the genes of histamine H2 receptor (HRH2), serotonin receptor (HTR2A1 and HTR2A2), and beta(3) adrenergic receptor (ADRB3). The method combines the high specificity of allele discrimination by oligonuc...
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PMID: 19026982
PDF is available here.
Abstract
We investigated whether NaB administered in combination with estradiol benzoate (EB) exerted antidepressant-like effect in forced swimming test (FST) in ovariectomized female rats. Furthermore, we detected the mRNA expressions of serotonin receptors and neuropeptides in hypothalamus, both of which p...
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PMID: 18817816
PDF is available here.
Abstract
The goal of this work was to study possible mechanisms underlying the potentiation of vasopressor response to serotonin observed in traumatic shock. Experiments with isolated aorta and mesenteric artery of the rat showed that vasoconstriction is caused by the activation of 5HT2A receptors. Agonists...
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PMID: 19548619
PDF is available here.
Abstract
We examine, as a predictor of depressive symptoms, the interaction between a single nucleotide polymorphism in the 2A receptor in the serotonin system (-1438G/A) and cultural consonance in family life, a measure of the degree to which an individual perceives her family as corresponding to a widely s...
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PMID: 18802937
PDF is available here.
Abstract
We observed that bilobalide significantly inhibited 5-HT-controlled egg-laying behavior in a dose-dependent manner, which was blocked in the 5-HT receptor mutants (ser-4, mod-1), but not in the 5-HT transporter (mod-5) or synthesis (tph-1) mutants. Bilobalide also potentiated a 5-HT-controlled, expe...
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PMID: 19545409
PDF is available here.
Abstract
The average difference in the binding potential (BPND) as measured on the two occasions in the frontal and temporal cortical regions ranged between 2 and 12%, with the lowest intraclass correlation coefficient in anterior cingulate regions. CONCLUSION: We conclude that the test-retest variability of...
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PMID: 19580676
PDF is available here.
Abstract
Our data constitutes the first report of direct involvement of 5-HT in human breast cancer. Increased 5-HT biosynthetic capacity accompanied by multiple changes in 5-HT receptor expression and signaling favor malignant progression of human breast cancer cells (for example, stimulated proliferation,...
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PMID: 19903352
PDF is available here.
Abstract
The rate at which the antidepressant drug is terminated and the duration of treatment appear to be key factors in predicting discontinuation symptoms. The development of animal models to explain the mechanisms of this clinical problem has proved challenging, because less than half of...
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PMID: 20214096
PDF is available here.