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Serotonin receptor subtype

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https://www.readbyqxmd.com/read/29116785/a-positive-allosteric-modulator-of-the-serotonin-5-ht2c-receptor-for-obesity
#1
Javier García Cárceles, Juan M Decara, Henar Vázquez-Villa, Ramón Rodríguez, Eva Codesido, Jacobo Cruces, José M Brea, María I Loza, Francisco Alén, Joaquin Botta, Peter J McCormick, Juan A Ballesteros, Bellinda Benhamú, Fernando Rodriguez de Fonseca, María L López-Rodrí Guez
The 5-HT2CR agonist lorcaserin, clinically approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer anti-obesity drugs, a chemical library from Vivia Biotech was screened using ExviTech® platform. Structural modifications of identified hit VA240 in synthesized analogues 6-41 afforded compound 11 (N-[(1-benzyl-1H-indol-3-yl)methyl]pyridin-3-amine, VA012), which exhibited dose-dependent enhancement of serotonin efficacy, no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands...
November 8, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29111111/anti-aggregation-effect-of-aroxyalkyl-derivatives-of-2-methoxyphenylpiperazine-is-due-to-their-5-ht2a-and-%C3%AE-2-adrenoceptor-antagonistic-properties-a-comparison-with-ketanserin-sarpogrelate-prazosin-yohimbine-and-arc239
#2
Monika Kubacka, Grzegorz Kazek, Magdalena Kotańska, Barbara Filipek, Anna Maria Waszkielewicz, Szczepan Mogilski
Serotonin (5-HT) and adrenaline acting at platelet 5-HT2A-serotoninergic and α2-adrenergic receptors are involved in platelet aggregation. We have evaluated the antagonistic potency at 5-HT2A, α2A-, and α2B-adrenoceptors as well as an anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and compared them with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239 (2-[2-[4-(o-methoxyphenyl)-piperazin-1-yl]-ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione). Functional bioassays at cells expressing human receptors, revealed studied compounds to be moderate antagonists of 5-HT2A and α2-adrenoceptors, with around 2-7 times stronger antagonistic effect at α2B subtype than α2A subtype...
October 27, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29101650/regulation-of-bone-metabolism-by-serotonin
#3
Brigitte Lavoie, Jane B Lian, Gary M Mawe
The processes of bone growth and turnover are tightly regulated by the actions of various signaling molecules, including hormones, growth factors, and cytokines. Imbalances in these processes can lead to skeletal disorders such as osteoporosis or high bone mass disease. It is becoming increasingly clear that serotonin can act through a number of mechanisms, and at different locations in the body, to influence the balance between bone formation and resorption. Its actions on bone metabolism can vary, based on its site of synthesis (central or peripheral) as well as the cells and subtypes of receptors that are activated...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29022279/the-role-of-%C3%AE-1-and-%C3%AE-2-adrenoceptor-subtypes-in-the-vasopressor-responses-induced-by-dihydroergotamine-in-ritanserin-pretreated-pithed-rats
#4
Eduardo Rivera-Mancilla, Victor H Avilés-Rosas, Guadalupe Manrique-Maldonado, Alain H Altamirano-Espinoza, Belinda Villanueva-Castillo, Antoinette MaassenVanDenBrink, Carlos M Villalón
BACKGROUND: Dihydroergotamine (DHE) is an acute antimigraine agent that displays affinity for dopamine D2-like receptors, serotonin 5-HT1/2 receptors and α1/α2-adrenoceptors. Since activation of vascular α1/α2-adrenoceptors results in systemic vasopressor responses, the purpose of this study was to investigate the specific role of α1- and α2-adrenoceptors mediating DHE-induced vasopressor responses using several antagonists for these receptors. METHODS: For this purpose, 135 male Wistar rats were pithed and divided into 35 control and 100 pretreated i...
October 11, 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28987939/a-hypothalamo-midbrain-medullary-pathway-involved-in-the-inhibition-of-the-respiratory-chemoreflex-response-induced-by-potassium-cyanide-in-rodents
#5
Tabinda Zafar, Charly Brouillard, Laurence Lanfumey, Caroline Sévoz-Couche
Recent studies have demonstrated that a mild stimulation of the dorsomedian nucleus of the hypothalamus (DMH), a defense area, induces the inhibition of the carotid chemoreflex tachypnea. DMH activation reduces the cardiac chemoreflex response via the dorsolateral part of the periaqueductal grey matter (dlPAG) and serotonin receptors (5-HT3 subtype) in the nucleus tractus solitarius (NTS). The objectives of this study were to assess whether dlPAG and subsequent NTS 5-HT3 receptors are involved in chemoreflex tachypnea inhibition during mild activation of the DMH...
October 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28987281/the-effects-of-the-5-ht7-receptor-on-hippocampal-long-term-potentiation-and-apoptosis-in-a-rat-model-of-alzheimer-s-disease
#6
Nasrin Hashemi-Firouzi, Alireza Komaki, Sara Soleimani Asl, Siamak Shahidi
Alzheimer's disease (AD) is the most common neurodegenerative disorder involving synaptic loss and impairments in learning and memory. Long-term potentiation (LTP) of synaptic function is a model of learning- and memory-related neural plasticity, of which serotonin (5-HT) is a key modulator in the hippocampus. As the 5-HT7 receptor subtype is implicated in hippocampal neuronal function, dendritic rearrangement, and neurogenesis, the aim of this study was to assess the effect of 5-HT7 receptor activation on hippocampal synaptic plasticity and apoptosis in a rat model of AD...
October 5, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28983239/the-serotonin-receptor-subtype-5b-specifically-interacts-with-serotonin-receptor-subtype-1a
#7
Sabine Niebert, Gijsbert J van Belle, Steffen Vogelgesang, Till Manzke, Marcus Niebert
Previously, we described the dysregulation of serotonin (5-HT) receptor subtype 5b (5-ht5b) in a mouse model of Rett syndrome (RTT). 5-ht5b has not been extensively studied, so we set out to characterize it in more detail. Unlike common cell surface receptors, 5-ht5b displays no membrane expression, while receptor clusters are located in endosomes. This unusual subcellular localization is at least in part controlled by glycosylation of the N-terminus, with 5-ht5b possessing fewer glycosylation sites than related receptors...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28965530/drugs-for-psychosis-and-mood-unique-actions-at-d3-d2-and-d1-dopamine-receptor-subtypes
#8
Stephen M Stahl
Drugs for psychosis and mood that bind dopamine D2 receptors can be classified not only by whether they also block serotonin 2A receptors, but by whether they also bind D3 or D1 receptors.
October 2017: CNS Spectrums
https://www.readbyqxmd.com/read/28920103/existence-of-brain-5-ht1a-5-ht2a-isoreceptor-complexes-with-antagonistic-allosteric-receptor-receptor-interactions-regulating-5-ht1a-receptor-recognition
#9
Dasiel O Borroto-Escuela, Xiang Li, Alexander O Tarakanov, David Savelli, Manuel Narváez, Kirill Shumilov, Yuniesky Andrade-Talavera, Antonio Jimenez-Beristain, Bartosz Pomierny, Zaida Díaz-Cabiale, Riccardo Cuppini, Patrizia Ambrogini, Maria Lindskog, Kjell Fuxe
Studies on serotonin-selective reuptake inhibitors have established that disturbances in the ascending 5-HT neuron systems and their 5-HT receptor subtypes and collateral networks to the forebrain contribute to the etiology of major depression and are targets for treatment. The therapeutic action of serotonin-selective reuptake inhibitors is of proven effectiveness, but the mechanisms underlying their effect are still unclear. There are many 5-HT subtypes involved; some need to be blocked (e.g., 5-HT2A, 5-HT3, and 5-HT7), whereas others need to be activated (e...
August 31, 2017: ACS Omega
https://www.readbyqxmd.com/read/28912689/monoamine-release-in-the-cat-lumbar-spinal-cord-during-fictive-locomotion-evoked-by-the-mesencephalic-locomotor-region
#10
Brian R Noga, Riza P Turkson, Songtao Xie, Annette Taberner, Alberto Pinzon, Ian D Hentall
Spinal cord neurons active during locomotion are innervated by descending axons that release the monoamines serotonin (5-HT) and norepinephrine (NE) and these neurons express monoaminergic receptor subtypes implicated in the control of locomotion. The timing, level and spinal locations of release of these two substances during centrally-generated locomotor activity should therefore be critical to this control. These variables were measured in real time by fast-cyclic voltammetry in the decerebrate cat's lumbar spinal cord during fictive locomotion, which was evoked by electrical stimulation of the mesencephalic locomotor region (MLR) and registered as integrated activity in bilateral peripheral nerves to hindlimb muscles...
2017: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/28901281/review-5-ht1-5-ht2-5-ht3-and-5-ht7-receptors-and-their-role-in-the-modulation-of-pain-response-in-the-central-nervous-system
#11
José Luis Cortes-Altamirano, Adriana Olmos-Hernández, Herlinda Bonilla-Jaime, Paul Carrillo-Mora, Cindy Bandala, S Reyes-Long, Alfonso Alfaro-Rodríguez
BACKGROUND: The aim of this review was to identify the mechanisms by which serotonin receptors involved at the central level are able to modulate the nociceptive response. Pain is a defense mechanism of the body that entails physiological, anatomical, neurochemical, and psychological changes, and is defined as an unpleasant sensory and emotional experience with potential risk of tissue damage, comprising the leading cause of appointments with Physicians worldwide. Treatment for this symptom has generated several neuropharmacological lines of research, due to the different types of pain and the various drugs employed to treat this condition...
September 11, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28899729/serotonin-gating-of-cortical-and-thalamic-glutamate-inputs-onto-principal-neurons-of-the-basolateral-amygdala
#12
Ji-Dong Guo, Brendan M O'Flaherty, Donald G Rainnie
The basolateral amygdala (BLA) is a key site for crossmodal association of sensory stimuli and an important relay in the neural circuitry of emotion. Indeed, the BLA receives substantial glutamatergic inputs from multiple brain regions including the prefrontal cortex and thalamic nuclei. Modulation of glutamatergic transmission in the BLA regulates stress- and anxiety-related behaviors. Serotonin (5-HT) also plays an important role in regulating stress-related behavior through activation of both pre- and postsynaptic 5-HT receptors...
November 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28855875/therapeutic-potential-of-selectively-targeting-the-%C3%AE-2c-adrenoceptor-in-cognition-depression-and-schizophrenia-new-developments-and-future-perspective
#13
REVIEW
Madeleine Monique Uys, Mohammed Shahid, Brian Herbert Harvey
α2A- and α2C-adrenoceptors (ARs) are the primary α2-AR subtypes involved in central nervous system (CNS) function. These receptors are implicated in the pathophysiology of psychiatric illness, particularly those associated with affective, psychotic, and cognitive symptoms. Indeed, non-selective α2-AR blockade is proposed to contribute toward antidepressant (e.g., mirtazapine) and atypical antipsychotic (e.g., clozapine) drug action. Both α2C- and α2A-AR share autoreceptor functions to exert negative feedback control on noradrenaline (NA) release, with α2C-AR heteroreceptors regulating non-noradrenergic transmission (e...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28826537/actions-and-regulation-of-ionotropic-cannabinoid-receptors
#14
Luciano De Petrocellis, Massimo Nabissi, Giorgio Santoni, Alessia Ligresti
Almost three decades have passed since the identification of the two specific metabotropic receptors mediating cannabinoid pharmacology. Thereafter, many cannabinoid effects, both at central and peripheral levels, have been well documented and characterized. However, numerous evidences demonstrated that these pharmacological actions could not be attributable solely to the activation of CB1 and CB2 receptors since several important cannabimimetic actions have been found in biological systems lacking CB1 or CB2 gene such as in specific cell lines or transgenic mice...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28818718/template-selection-and-refinement-considerations-for-modelling-aminergic-gpcr-ligand-complexes
#15
Kaniz F Urmi, Angela M Finch, Renate Griffith
G protein-coupled receptors (GPCRs) are important targets for development of drugs for the treatment of many diseases. However, crystal structures are available for only a small fraction of these membrane bound proteins. Accurate homology models will provide opportunities for effective drug design targeting GPCRs. Recently, several serotonin receptor crystal structures were solved and needed to be evaluated as potential templates. In the first part of this work different measures of similarity in template selection were explored and methods for homology modelling, docking and refinement of aminergic GPCR-ligand complexes were developed and evaluated by comparing models of the D3-R/eticlopride complex with the crystal structure...
September 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28765614/hierarchy-in-the-home-cage-affects-behaviour-and-gene-expression-in-group-housed-c57bl-6-male-mice
#16
Yasuyuki Horii, Tatsuhiro Nagasawa, Hiroyuki Sakakibara, Aki Takahashi, Akira Tanave, Yuki Matsumoto, Hiromichi Nagayama, Kazuto Yoshimi, Michiko T Yasuda, Kayoko Shimoi, Tsuyoshi Koide
Group-housed male mice exhibit aggressive behaviour towards their cage mates and form a social hierarchy. Here, we describe how social hierarchy in standard group-housed conditions affects behaviour and gene expression in male mice. Four male C57BL/6 mice were kept in each cage used in the study, and the social hierarchy was determined from observation of video recordings of aggressive behaviour. After formation of a social hierarchy, the behaviour and hippocampal gene expression were analysed in the mice. Higher anxiety- and depression-like behaviours and elevated gene expression of hypothalamic corticotropin-releasing hormone and hippocampal serotonin receptor subtypes were observed in subordinate mice compared with those of dominant mice...
August 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28762314/insights-into-nicotinic-receptor-signaling-in-nicotine-addiction-implications-for-prevention-and-treatment
#17
Wuyi Liu, Ming D Li
Nicotinic acetylcholine receptors (nAChRs) belong to the Cys-loop ligand-gated ion-channel (LGIC) superfamily, which also includes the GABA, glycine, and serotonin receptors. Many nAChR subunits have been identified and shown to be involved in signal transduction on binding to them of either the neurotransmitter acetylcholine or exogenous ligands such as nicotine. The nAChRs are pentameric assemblies of homologous subunits surrounding a central pore that gates cation flux, and they are expressed at neuromuscular junctions throughout the nervous system...
August 1, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28745513/modulating-the-serotonin-receptor-spectrum-of-pulicatin-natural-products
#18
Zhenjian Lin, Misty D Smith, Gisela P Concepcion, Margo G Haygood, Baldomero M Olivera, Alan Light, Eric W Schmidt
Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure-activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore...
August 25, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28729057/neuropathic-pain-alleviating-effects-of-pyrazole-conjugated-arylsulfonamides-as-5-ht6-receptor-antagonists
#19
Jin Ri Hong, Hyunah Choo, Ghilsoo Nam
A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. We also investigated their neuropathic pain-alleviating effects in vivo using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT6 inhibitory activity in vitro. Among them, selected compounds, 12 and 13, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28726540/mechanisms-of-the-analgesic-effect-of-calcitonin-on-chronic-pain-by-alteration-of-receptor-or-channel-expression
#20
Akitoshi Ito, Megumu Yoshimura
The polypeptide hormone calcitonin is well known clinically for its ability to relieve osteoporotic back pain and neuropathic pain such as spinal canal stenosis, diabetic neuropathy, chemotherapy-induced neuropathy, and complex regional pain syndrome. Because the analgesic effects of calcitonin have a broad range, the underlying mechanisms of pain relief by calcitonin are largely unknown. However, recent studies using several types of chronic pain models combined with various methods have been gradually clarifying the mechanism...
January 2017: Molecular Pain
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