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Serotonin receptor subtype

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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
#1
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
#2
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
#3
Cortes-Altamirano José Luis, Olmos-Hernández Adriana, Bonilla-Jaime Herlinda, Carrillo-Mora Paul, Bandala Cindy, S Reyes-Long, Alfaro-Rodríguez Alfonso
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
#4
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...
September 9, 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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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...
July 26, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28729057/neuropathic-pain-alleviating-effects-of-pyrazole-conjugated-arylsulfonamides-as-5-ht6-receptor-antagonists
#11
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
#12
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
https://www.readbyqxmd.com/read/28720013/the-5-ht1b-serotonin-receptor-regulates-methylphenidate-induced-gene-expression-in-the-striatum-differential-effects-on-immediate-early-genes
#13
David Alter, Joel A Beverley, Ronak Patel, Carlos A Bolaños-Guzmán, Heinz Steiner
Drug combinations that include a psychostimulant such as methylphenidate (Ritalin) and a selective serotonin reuptake inhibitor such as fluoxetine are indicated in several medical conditions. Co-exposure to these drugs also occurs with "cognitive enhancer" use by individuals treated with selective serotonin reuptake inhibitors. Methylphenidate, a dopamine reuptake inhibitor, by itself produces some addiction-related gene regulation in the striatum. We have demonstrated that co-administration of selective serotonin reuptake inhibitors potentiates these methylphenidate-induced molecular effects, thus producing a more "cocaine-like" profile...
August 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28711602/contribution-of-5-ht2a-receptors-on-diaphragmatic-recovery-after-chronic-cervical-spinal-cord-injury
#14
Kun-Ze Lee, Elisa J Gonzalez-Rothi
Unilateral C2 spinal cord hemisection (C2Hx) interrupts bulbospinal respiratory pathways innervating ipsilateral phrenic motoneurons, resulting in cessation of ipsilateral diaphragm motor output. Plasticity within the spinal neural circuitry controlling the diaphragm can induce partial recovery of phrenic bursting which correlates with the time-dependent return of spinal serotonin (5-HT) immunoreactivity in the vicinity of phrenic motoneurons. The 5-HT2A receptor subtype is present on phrenic motoneurons and its expression is up-regulated after cervical spinal cord injury; however the functional role of these receptors following injury has not been clearly defined...
July 12, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28677096/hallucinogens-and-serotonin-5-ht2a-receptor-mediated-signaling-pathways
#15
Juan F López-Giménez, Javier González-Maeso
The neuropsychological effects of naturally occurring psychoactive chemicals have been recognized for millennia. Hallucinogens, which include naturally occurring chemicals such as mescaline and psilocybin, as well as synthetic compounds, such as lysergic acid diethylamide (LSD), induce profound alterations of human consciousness, emotion, and cognition. The discovery of the hallucinogenic effects of LSD and the observations that LSD and the endogenous ligand serotonin share chemical and pharmacological profiles led to the suggestion that biogenic amines like serotonin were involved in the psychosis of mental disorders such as schizophrenia...
July 5, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28676029/cardiovascular-concern-of-5-ht2b-receptor-and-recent-vistas-in-the-development-of-its-antagonists
#16
Komal Padhariya, Richie R Bhandare, Daniel Canney, Vinay Velingkar
The serotonin 2B receptor subtype (5-HT2BR), located in central nervous system (CNS), cardiovascular system (CVS) and the gastrointestinal tract (GIT), is an important target for the treatment of migraine, obesity and irritable bowel syndrome. 5-HT2BR is necessary for the myocardial cell proliferation and differentiation at the embroyonic stage for healthy development of heart. Recently, its involvement in drug induced valvulopathy and other myocardial disorders have paved a way for selective antagonist for the treatment of cardiac disorders...
July 3, 2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28647411/hippocampal-5-ht1a-receptor-expression-changes-in-prodromal-stages-of-alzheimer-s-disease-beneficial-or-deleterious
#17
REVIEW
Mathieu Verdurand, Luc 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
#18
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 behavior. Although the serotonin system has been implicated in modulating empathy and moral behavior, the relative contribution of the various serotonin receptor subtypes is still unknown. Methods: We investigated the acute effect of psilocybin (0...
September 1, 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
#19
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...
August 1, 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
#20
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
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