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Serotonin receptor subtype

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https://www.readbyqxmd.com/read/28647411/hippocampal-5-ht1a-receptor-expression-changes-in-prodromal-stages-of-alzheimer-s-disease-beneficial-or-deleterious
#1
REVIEW
M Verdurand, L Zimmer
There is increasing evidence that the serotonergic system is highly dysfunctional in Alzheimer's disease (AD), and this could be related to cognitive impairments associated with dementia. Of the various serotonin receptors, 5-HT1A receptors are relevant to AD as they are highly expressed in the human hippocampus and are known to be involved in the regulation of memory processes. This review will discuss the involvement of 5-HT1A receptors in AD at several levels (post-mortem, in-vivo imaging, animal models)...
June 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#2
Thomas Pokorny, Katrin H Preller, Michael Kometer, Isabel Dziobek, Franz X Vollenweider
Background: Impaired empathic abilities lead to severe negative social consequences and influence the development and treatment of several psychiatric disorders. Furthermore, empathy has been shown to play a crucial role in moral and prosocial behaviour. Although the serotonin (5-HT) system has been implicated in modulating empathy and moral behaviour, the relative contribution of the various 5-HT receptor subtypes is still unknown. Methods: We investigated the acute effect of psilocybin (0...
June 16, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28606760/progress-in-the-discovery-of-small-molecule-modulators-of-the-cys-loop-superfamily-receptors
#3
REVIEW
Brian A Sparling, Erin F DiMauro
The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), γ-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Here, we review efforts to discover selective small molecules targeting one or more Cys-loop receptors, with a focus on state-of-the-art modulators that have been reported over the past five years. Several highlighted compounds offer robust oral bioavailability and central exposure and have thus been useful in delineating pharmacokinetic/pharmacodynamic relationships in pre-clinical disease models...
May 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28606116/characterization-of-serotonin-induced-inhibition-of-excitatory-synaptic-transmission-in-the-anterior-cingulate-cortex
#4
Zhen Tian, Manabu Yamanaka, Matteo Bernabucci, Ming-Gao Zhao, Min Zhuo
Excitatory synaptic transmission in central synapses is modulated by serotonin (5-HT). The anterior cingulate cortex (ACC) is an important cortical region for pain perception and emotion. ACC neurons receive innervation of projecting serotonergic nerve terminals from raphe nuclei, but the possible effect of 5-HT on excitatory transmission in the ACC has not been investigated. In the present study, we investigated the role of 5-HT on glutamate neurotransmission in the ACC slices of adult mice. Bath application of 5-HT produced dose-dependent inhibition of evoked excitatory postsynaptic currents (eEPSCs)...
June 12, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28597539/developmental-effects-of-antipsychotic-drugs-on-serotonin-receptor-subtypes
#5
Yong Kee Choi, Matthew P Gardner, Frank I Tarazi
Antipsychotic medications are increasingly prescribed to pediatric and adolescent patients with psychotic diseases in spite of limited knowledge on the long-term effects of dissimilar antipsychotic drugs on developing brain. In this study, we quantified the levels of two major serotonin 5-HT1A , and 5-HT2A receptors in brain regions of developing rats after 3 weeks of treatment with typical (fluphenazine) and atypical (clozapine and olanzapine) antipsychotics, and compared to similarly treated adult rats treated with olanzapine, risperidone and quetiapine examined in previous studies...
June 8, 2017: Synapse
https://www.readbyqxmd.com/read/28587819/prodepressant-and-anxiogenic-like-effects-of-serotonin-selective-but-not-noradrenaline-selective-antidepressant-agents-in-mice-lacking-%C3%AE-2-containing-gabaa-receptors
#6
Rebecca S Benham, Nishani B Hewage, Raymond F Suckow, Elif Engin, Uwe Rudolph
Deficits in neuronal inhibition via gamma-aminobutyric acid (GABA) type A receptors (GABAA-Rs) are implicated in the pathophysiology of major depressive disorder and the therapeutic effects of current antidepressant treatments, however, the relevant GABAA-R subtype as defined by its alpha subunit is still unknown. We previously reported anxiety- and depressive-like behavior in alpha2+/- and alpha2-/- mice, respectively (Vollenweider, 2011). We sought to determine whether this phenotype could be reversed by chronic antidepressant treatment...
June 3, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28559799/the-effect-of-serotonin-targeting-antidepressants-on-neurogenesis-and-neuronal-maturation-of-the-hippocampus-mediated-via-5-ht1a-and-5-ht4-receptors
#7
REVIEW
Eri Segi-Nishida
Antidepressant drugs such as selective serotonin reuptake inhibitors (SSRIs) specifically increase serotonin (5-HT) levels in the synaptic cleft and are widely used to treat mood and anxiety disorders. There are 14 established subtypes of 5-HT receptors in rodents, each of which has regionally different expression patterns. Many preclinical studies have suggested that the hippocampus, which contains abundant 5-HT1A and 5-HT4 receptor subtypes in the dentate gyrus (DG), is critically involved in the mechanisms of action of antidepressants...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28555112/caveolin-1-functional-insights-into-its-role-in-muscarine-and-serotonin-induced-smooth-muscle-constriction-in-murine-airways
#8
Maryam Keshavarz, Heike Schwarz, Petra Hartmann, Silke Wiegand, Melanie Skill, Mike Althaus, Wolfgang Kummer, Gabriela Krasteva-Christ
An increased bronchoconstrictor response is a hallmark in the progression of obstructive airway diseases. Acetylcholine and 5-hydroxytryptamine (5-HT, serotonin) are the major bronchoconstrictors. There is evidence that both cholinergic and serotonergic signaling in airway smooth muscle (ASM) involve caveolae. We hypothesized that caveolin-1 (cav-1), a structural protein of caveolae, plays an important regulatory role in ASM contraction. We analyzed airway contraction in different tracheal segments and extra- and intrapulmonary bronchi in cav-1 deficient (cav-1-/-) and wild-type mice using organ bath recordings and videomorphometry of methyl-beta-cyclodextrin (MCD) treated and non-treated precision-cut lung slices (PCLS)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28553207/dm5-ht2b-pharmacological-characterization-of-the-fifth-serotonin-receptor-subtype-of-drosophila-melanogaster
#9
Wolfgang Blenau, Stöppler Daniel, Sabine Balfanz, Markus Thamm, Arnd Baumann
Serotonin (5-hydroxytryptamine, 5-HT) is an important regulator of physiological and behavioral processes in both protostomes (e.g., insects) and deuterostomes (e.g., mammals). In insects, serotonin has been found to modulate the heart rate and to control secretory processes, development, circadian rhythms, aggressive behavior, as well as to contribute to learning and memory. Serotonin exerts its activity by binding to and activating specific membrane receptors. The clear majority of these receptors belong to the superfamily of G-protein-coupled receptors...
2017: Frontiers in Systems Neuroscience
https://www.readbyqxmd.com/read/28553205/dopamine-and-serotonin-induced-modulation-of-gabaergic-and-glutamatergic-transmission-in-the-striatum-and-basal-forebrain
#10
REVIEW
Toshihiko Momiyama, Takuma Nishijo
Catecholamine receptor-mediated modulation of glutamatergic or GABAergic transmission in the striatum as well as basal forebrain (BF) has been intensively studied during these two decades. In the striatum, activation of dopamine (DA) D2 receptors in GABAergic terminals inhibits GABA release onto cholinergic interneurons by selective blockade of N-type calcium channels. In the BF, glutamatergic transmission onto cholinergic projection neurons is inhibited via DA D1-like receptors by selective blockade of P/Q-type calcium channels...
2017: Frontiers in Neuroanatomy
https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#11
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
May 25, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28544903/estrogen-receptor-%C3%AE-deficiency-impairs-bdnf-5-ht2a-signaling-in-the-hippocampus-of-female-brain-a-possible-mechanism-for-menopausal-depression
#12
Anindit Chhibber, Sarah K Woody, M A Karim Rumi, Michael J Soares, Liqin Zhao
Depression currently affects 350 million people worldwide and 19 million Americans each year. Women are 2.5 times more likely to experience major depression than men, with some women appearing to be at a heightened risk during the menopausal transition. Estrogen signaling has been implicated in the pathophysiology of mood disorders including depression; however, the underlying mechanisms are poorly understood. In this study, the role of estrogen receptor (ER) subtypes, ERα and ERβ, in the regulation of brain-derived neurotrophic factor (BDNF) and serotonin (5-HT) signaling was investigated; two pathways that have been hypothesized to be interrelated in the etiology of depression...
May 18, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28483714/purposeless-oral-activity-induced-by-meta-chlorophenylpiperazine-m-cpp-undefined-tic-like-behaviors
#13
Deborah S Kreiss, Philippe De Deurwaerdère
BACKGROUND: The pathophysiological hypothesis underlying tic disorders in Tourette syndrome (TS) is that basal ganglia are not capable of properly filtering cortical information, leading patients with difficulties in inhibiting unwanted behaviors or impulses. One of the main challenges for furthering such a hypothesis is to find appropriate animal models summarizing some aspects of the disease. METHODS: It has been established for more than 25 years in rodents that the prototypical serotonin (5-HT) agonist meta-chlorophenylpiperazine (m-CPP) elicits purposeless oral movements including chewing behavior...
May 5, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28483393/activation-of-5-ht7-receptors-reverses-nmda-r-dependent-ltd-by-activating-pka-in-medial-vestibular-neurons
#14
Yan-Hai Li, Lei Han, Kenneth Lap-Kei Wu, Ying-Shing Chan
The medial vestibular nucleus (MVN) is a major output station for neurons that project to the vestibulo-spinal pathway. MVN neurons show capacity for long-term depression (LTD) during the juvenile period. We investigated LTD of MVN neurons using whole-cell patch-clamp recordings. High frequency stimulation (HFS) robustly induced LTD in 90% of type B neurons in the MVN, while only 10% of type A neurons were responsive, indicating that type B neurons are the major contributors to LTD in the MVN. The neuromodulator serotonin (5-HT) is known to modulate LTD in neural circuits of the cerebral cortex and the hippocampus...
May 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28459524/growing-evidence-for-heterogeneous-synaptic-localization-of-5-ht2a-receptors
#15
Carine Bécamel, Coralie Berthoux, Alexander Barre, Philippe Marin
The serotonin 2A (5-HT2A) receptor subtype continues to attract attention as a target for numerous psychoactive drugs including psychedelic hallucinogens, antidepressants, anxiolytics, and atypical antipsychotics. 5-HT2A receptors are a principal G protein-coupled receptor subtype mediating the excitatory effects of serotonin. Nonetheless, pre- vs postsynaptic localization of 5HT2A receptors, relative to glutamatergic synapses, has remained controversial. Here, we discuss recent findings highlighting the existence and roles of presynaptic 5-HT2A receptors in regulating glutamatergic transmission and cognition...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28458330/gender-differences-in-serotonin-signaling-in-patients-with-diarrhea-predominant-irritable-bowel-syndrome
#16
Ryo Katsumata, Akiko Shiotani, Takahisa Murao, Manabu Ishii, Minoru Fujita, Hiroshi Matsumoto, Ken Haruma
Objective Gender differences, including differences in the prevalence, subtypes and the effectiveness of treatment, are generally recognized in irritable bowel syndrome (IBS). Although serotonin type 3 receptor (5-HT3R) antagonists appear to be more effective in women with diarrhea predominant IBS (IBS-D) than they are in men, the mechanisms underlying these effects remain unclear. The aim of the present was to investigate the gender differences in 5-HT signaling. Methods The subjects were selected from outpatients with IBS-D and healthy controls...
2017: Internal Medicine
https://www.readbyqxmd.com/read/28414989/role-of-cortical-alpha-2-adrenoceptors-in-alcohol-withdrawal-induced-depression-and-tricyclic-antidepressants
#17
Bruk Getachew, Sheketha R Hauser, Antonei B Csoka, Robert E Taylor, Yousef Tizabi
INTRODUCTION: Although a role for alpha-2 adrenoceptors (alpha-2 ARs) in alcohol use disorder (AUD) and depression is suggested, very little information on a direct interaction between alcohol and these receptors is available. METHODS: In this study adult female Wistar and Wistar-Kyoto (WKY) rats, a putative animal model of depression, were exposed to alcohol vapor 3h daily for 10days (blood alcohol concentration ∼150mg%) followed by daily injection of 10mg/kg of imipramine (IMP, a selective norepinephrine NE/serotonin reuptake inhibitor) or nomifensine (NOMI, a selective NE/dopamine reuptake inhibitor)...
June 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28404880/serotonergic-system-antagonists-target-breast-tumor-initiating-cells-and-synergize-with-chemotherapy-to-shrink-human-breast-tumor-xenografts
#18
William D Gwynne, Robin M Hallett, Adele Girgis-Gabardo, Bojana Bojovic, Anna Dvorkin-Gheva, Craig Aarts, Kay Dias, Anita Bane, John A Hassell
Breast tumors comprise an infrequent tumor cell population, termed breast tumor initiating cells (BTIC), which sustain tumor growth, seed metastases and resist cytotoxic therapies. Hence therapies are needed to target BTIC to provide more durable breast cancer remissions than are currently achieved. We previously reported that serotonergic system antagonists abrogated the activity of mouse BTIC resident in the mammary tumors of a HER2-overexpressing model of breast cancer. Here we report that antagonists of serotonin (5-hydroxytryptamine; 5-HT) biosynthesis and activity, including US Federal Food and Drug Administration (FDA)-approved antidepressants, targeted BTIC resident in numerous breast tumor cell lines regardless of their clinical or molecular subtype...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28361518/ketanserin-and-naftopidil-enhance-the-potentiating-effect-of-alpha-methyl-serotonin-on-the-neurally-induced-contraction-of-human-isolated-urinary-bladder-muscle-strips
#19
Tsuyoshi Hattori, Philippe Lluel, Céline Rouget, Moèz Rekik, Mitsuharu Yoshiyama
PURPOSE: The aim of this study was to assess the potential involvement of a specific subtype of 5-hydroxytryptamine (5-HT), 5HT2 receptors in neurally-induced contractions of the human detrusor. METHODS: Contractile responses to electrical field stimulation (EFS) were examined in human isolated urinary bladder muscle strips. The potentiation of EFS-induced detrusor contraction was examined by adding cumulative concentrations of a 5-HT and 5-HT2 receptor agonist, α-methyl-serotonin (α-Me-5-HT) (1nM-100μM) in the presence or absence of a 5-HT2 antagonist, ketanserin (5-HT2A>5-HT2C) or naftopidil (5-HT2B>5-HT2A) (0...
March 24, 2017: International Neurourology Journal
https://www.readbyqxmd.com/read/28322152/serotonin-receptor-binding-characteristics-of-geissoschizine-methyl-ether-an-indole-alkaloid-in-uncaria-hook
#20
Yasushi Ikarashi, Kyoji Sekiguchi, Kazushige Mizoguchi
Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes. Here we describe previous findings and our own data to review the binding characteristics of GM to the 5-HT receptor subtypes. Competitive receptor-binding assays showed that GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4, 5-HT5A, 5-HT6, and 5-HT7...
March 20, 2017: Current Medicinal Chemistry
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