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Serotonin receptor subtype

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https://www.readbyqxmd.com/read/29766792/gabaa-receptors-various-stoichiometrics-of-subunit-arrangement-in-%C3%AE-1%C3%AE-3-and-%C3%AE-1%C3%AE-3%C3%AE%C2%B5-receptors
#1
Ahmad Tarmizi Che Has, Mary Chebib
GABAA receptors (GABAARs) are members of the Cys-loop ligand-gated ion channel (LGIC) superfamily, which includes nicotinic acetylcholine, glycine, and serotonin (5HT3) receptors [1,2,3,4]. LGICs typically mediate fast synaptic transmission via the movement of ions through channels gated by neurotransmitters, such as acetylcholine for nicotinic receptors and GABA for GABAARs [5]. The term Cys-loop receptors originates from the presence of a conserved disulphide bond (or bridge) which holds together two cysteine amino acids of the loop that forms from the structure of polypeptides in the extracellular domain of the receptor's subunit [6]...
May 15, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29763291/classics-in-neuroimaging-the-serotonergic-2a-receptor-system-from-discovery-to-modern-molecular-imaging
#2
Elina T L'Estrade, Hanne D Hansen, Maria Erlandsson, Tomas G Ohlsson, Gitte M Knudsen, Matthias M Herth
Already in 1953, Woolley and Shaw speculated that serotonin could be involved in a range of central nervous system (CNS) disorders. Lysergic acid diethylamide (LSD) displayed an important role in this respect. It was used not only to antagonize biological effects of serotonin and to study the system itself, but also to identify serotonergic subtype receptors. The 5-HT2A receptor was discovered in the 1970s and identified as the responsible receptor mediating psychedelic effects of LSD. The development of positron emission tomography (PET) allowed to study this receptor system in vivo...
May 15, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#3
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29706583/serotonergic-signaling-controls-input-specific-synaptic-plasticity-at-striatal-circuits
#4
Anna Cavaccini, Marta Gritti, Andrea Giorgi, Andrea Locarno, Nicolas Heck, Sara Migliarini, Alice Bertero, Maddalena Mereu, Giulia Margiani, Massimo Trusel, Tiziano Catelani, Roberto Marotta, Maria Antonietta De Luca, Jocelyne Caboche, Alessandro Gozzi, Massimo Pasqualetti, Raffaella Tonini
Monoaminergic modulation of cortical and thalamic inputs to the dorsal striatum (DS) is crucial for reward-based learning and action control. While dopamine has been extensively investigated in this context, the synaptic effects of serotonin (5-HT) have been largely unexplored. Here, we investigated how serotonergic signaling affects associative plasticity at glutamatergic synapses on the striatal projection neurons of the direct pathway (dSPNs). Combining chemogenetic and optogenetic approaches reveals that impeding serotonergic signaling preferentially gates spike-timing-dependent long-term depression (t-LTD) at thalamostriatal synapses...
April 25, 2018: Neuron
https://www.readbyqxmd.com/read/29679900/structural-insights-into-serotonin-receptor-ligands-polypharmacology
#5
Sabina Podlewska, Rafał Kafel, Enza Lacivita, Grzegorz Satała, Albert J Kooistra, Márton Vass, Chris de Graaf, Marcello Leopoldo, Andrzej J Bojarski, Stefan Mordalski
Identifying desired interactions with a target receptor is often the first step when designing new active compounds. However, attention should also be focused on contacts with other proteins that result in either selective or polypharmacological compounds. Here, the search for the structural determinants of selectivity between selected serotonin receptor subtypes was carried out. Special attention was focused on 5-HT7 R and the cross-interactions between its ligands and the 5-HT1A R, 5-HT1B R, 5-HT2A R, 5-HT2B R, and 5-HT6 R subtypes...
April 6, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29649585/effects-of-different-serotonin-receptor-subtype-antagonists-on-the-development-of-cardiac-allograft-vasculopathy-in-murine-aortic-allografts
#6
Annika Gocht, Jörg H W Distler, Bernd Spriewald, Martina Ramsperger-Gleixner, Michael Weyand, Stephan M Ensminger, Christian Heim
BACKGROUND: Cardiac allograft vasculopathy (CAV) is the main obstacle for long-term survival after heart transplantation. Alloimmune mediated chronic vascular rejection results in several mechanisms like platelet activation, immigration of inflammatory cells through the endothelial layer and proliferation and migration of smooth muscle cells (SMCs). Serotonin (5-HT) promotes these processes via activation of 5-HT2 receptors. We hypothesized that inhibiting 5-HT2 receptors ameliorates the development of CAV...
April 9, 2018: Transplant Immunology
https://www.readbyqxmd.com/read/29577069/identification-of-natural-products-as-novel-ligands-for-the-human-5-ht-2c-receptor
#7
Yao Peng, Simeng Zhao, Yiran Wu, Haijie Cao, Yueming Xu, Xiaoyan Liu, Wenqing Shui, Jianjun Cheng, Suwen Zhao, Ling Shen, Jun Ma, Ronald J Quinn, Raymond C Stevens, Guisheng Zhong, Zhi-Jie Liu
G protein-coupled receptors (GPCRs) constitute the largest human protein family with over 800 members, which are implicated in many important medical conditions. Serotonin receptors belong to the aminergic GPCR subfamily and play important roles in physiological and psychological activities. Structural biology studies have revealed the structures of many GPCRs in atomic details and provide the basis for the identification and investigation of the potential ligands, which interact with and modulate the receptors...
2018: Biophysics Reports
https://www.readbyqxmd.com/read/29572515/neuronal-differentiation-induces-snord115-expression-and-is-accompanied-by-post-transcriptional-changes-of-serotonin-receptor-2c-mrna
#8
Tomaž Bratkovič, Miha Modic, Germán Camargo Ortega, Micha Drukker, Boris Rogelj
The serotonin neurotransmitter system is widespread in the brain and implicated in modulation of neuronal responses to other neurotransmitters. Among 14 serotonin receptor subtypes, 5-HT2cR plays a pivotal role in controlling neuronal network excitability. Serotonergic activity conveyed through receptor 5-HT2cR is regulated post-transcriptionally via two mechanisms, alternative splicing and A-to-I RNA editing. Brain-specific small nucleolar RNA SNORD115 harbours a phylogenetically conserved 18-nucleotide antisense element with perfect complementarity to the region of 5ht2c primary transcript that undergoes post-transcriptional changes...
March 23, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29563831/serotonin-receptor-agonists-in-the-acute-treatment-of-migraine-a-review-on-their-therapeutic-potential
#9
REVIEW
Andrea Negro, Angela Koverech, Paolo Martelletti
Migraine is an important socioeconomic burden and is ranked the sixth cause of years of life lost because of disability in the general population and the third cause of years of life lost in people younger than 50 years. The cornerstone of pharmacological treatment is represented by the acute therapy. The serotonin (5-hydroxytryptamine [5-HT]) receptor subtype 1B /1D agonists, called triptans, are nowadays the first-line acute therapy for patients who experience moderate-to-severe migraine attacks. Unfortunately, a high percentage of patients are not satisfied with this acute treatment, either for lack of response or side effects...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29560272/crystal-structure-of-the-human-5-ht-1b-serotonin-receptor-bound-to-an-inverse-agonist
#10
Wanchao Yin, X Edward Zhou, Dehua Yang, Parker W de Waal, Meitian Wang, Antao Dai, Xiaoqing Cai, Chia-Ying Huang, Ping Liu, Xiaoxi Wang, Yanting Yin, Bo Liu, Yu Zhou, Jiang Wang, Hong Liu, Martin Caffrey, Karsten Melcher, Yechun Xu, Ming-Wei Wang, H Eric Xu, Yi Jiang
5-hydroxytryptamine (5-HT, also known as serotonin) regulates many physiological processes through the 5-HT receptor family. Here we report the crystal structure of 5-HT1B subtype receptor (5-HT1B R) bound to the psychotropic serotonin receptor inverse agonist methiothepin (MT). Crystallization was facilitated by replacing ICL3 with a novel optimized variant of BRIL (OB1) that enhances the formation of intermolecular polar interactions, making OB1 a potential useful tool for structural studies of membrane proteins...
2018: Cell Discovery
https://www.readbyqxmd.com/read/29523295/molecular-hypotheses-to-explain-the-shared-pathways-and-underlying-pathobiological-causes-in-catatonia-and-in-catatonic-presentations-in-neuropsychiatric-disorders
#11
E M Peter-Ross
The pathobiological causes, the shared cellular and molecular pathways in catatonia and in catatonic presentation in neuropsychiatric disorders are yet to be determined. The hypotheses in this paper have been deduced from the latest scientific research findings and clinical observations of patients with genetic disorders, behavioral phenotypes and other family members suffering mental disorders. The first hypothesis postulates that catatonia and the heterogeneity of catatonic signs and symptoms involve nucleolar dysfunction arising from abnormalities of the brain-specific, non-coding micro-RNA, SNORD115 genes (either duplications or deletions) which result in pathobiological dysfunction of various combinations in the downstream pathways (possibly along with other genes in these shared pathways)...
April 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29516301/convergent-mechanisms-underlying-rapid-antidepressant-action
#12
REVIEW
Panos Zanos, Scott M Thompson, Ronald S Duman, Carlos A Zarate, Todd D Gould
Traditional pharmacological treatments for depression have a delayed therapeutic onset, ranging from several weeks to months, and there is a high percentage of individuals who never respond to treatment. In contrast, ketamine produces rapid-onset antidepressant, anti-suicidal, and anti-anhedonic actions following a single administration to patients with depression. Proposed mechanisms of the antidepressant action of ketamine include N-methyl-D-aspartate receptor (NMDAR) modulation, gamma aminobutyric acid (GABA)-ergic interneuron disinhibition, and direct actions of its hydroxynorketamine (HNK) metabolites...
March 2018: CNS Drugs
https://www.readbyqxmd.com/read/29483349/benefits-and-limitations-of-drug-studies-in-temperament-research-biochemical-responses-as-indicators-of-temperament
#13
REVIEW
Petra Netter
This paper presents a discussion of principles and problems of neurotransmitter challenge tests using examples of experiments, most of which were performed in the author's laboratory. Drugs targeting synthesis, release, receptors or reuptake of dopamine, serotonin and noradrenergic transmitter (TM) systems were used for characterizing or discriminating certain temperament or personality traits and their sub-factors. Any personality or temperament trait is characterized by multiple TM responses, thus constellations of hormone responses to drugs acting on different TM systems or on different sources of TM activity were investigated within individuals in crossover designs...
April 19, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29471490/pharmacologic-assessment-of-bovine-ruminal-and-mesenteric-vascular-serotonin-receptor-populations
#14
Miriam A Snider, David L Harmon, James L Klotz
Prior work using a contractility bioassay determined that the serotonin (5-HT) receptor subtype 5-HT2A is present in bovine lateral saphenous veins and plays a role in ergot alkaloid (EA)-induced vascular contraction in steers grazing endophyte-infected (Epichloë coenophiala) tall fescue (Lolium arundinaceum). Ergot alkaloids have also been shown to be vasoactive in bovine gut vasculature. To determine what 5-HT receptors are involved in vasoconstriction of gut vasculature, contractility of ruminal and mesenteric arteries and veins collected from cattle was evaluated in the presence of agonists selective for 5-HT1B (CP 93129), 5-HT1D (L-694, 247), 5-HT2A (TCB-2), 5-HT2B (BW 723C86), 5-HT4 (BIMU-8), and 5-HT7 (LP 44) receptors...
April 14, 2018: Journal of Animal Science
https://www.readbyqxmd.com/read/29424302/the-role-of-5-ht1a-receptor-in-the-cancer-as-a-new-opportunity-in-medicinal-chemistry
#15
Angela Corvino, Ferdinando Fiorino, Beatrice Severino, Irene Saccone, Francesco Frecentese, Elisa Perissutti, Paola Di Vaio, Vincenzo Santagada, Giuseppe Caliendo, Elisa Magli
The 5-HT1A receptor is a pharmacologically well characterized serotonin receptor subtype and it has long been investigated because of its involvement in several physio-pathological mechanisms and treatment of neurological diseases like ansia and depression. Serotonin (5-HT) also shows many non-neural functions such as essential hypertension, embryogenesis, follicle maturation and behavior. Moreover it exerts a growth factor function on different types of non-tumoral cells, and it was also found to be related to oncogenes...
February 9, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29422840/mechanisms-underlying-serotonergic-excitation-of-callosal-projection-neurons-in-the-mouse-medial-prefrontal-cortex
#16
Emily K Stephens, Arielle L Baker, Allan T Gulledge
Serotonin (5-HT) selectively excites subpopulations of pyramidal neurons in the neocortex via activation of 5-HT2A (2A) receptors coupled to Gq subtype G-protein alpha subunits. Gq -mediated excitatory responses have been attributed primarily to suppression of potassium conductances, including those mediated by KV 7 potassium channels (i.e., the M-current), or activation of non-specific cation conductances that underlie calcium-dependent afterdepolarizations (ADPs). However, 2A-dependent excitation of cortical neurons has not been extensively studied, and no consensus exists regarding the underlying ionic effector(s) involved...
2018: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/29397535/the-leptin-dopamine-and-serotonin-receptors-in-hypothalamic-pomc-neurons-of-normal-and-obese-rodents
#17
Irina V Romanova, Kira V Derkach, Anastasiya L Mikhrina, Ivan B Sukhov, Elena V Mikhailova, Alexander O Shpakov
The pro-opiomelanocortin (POMC)-expressing neurons of the hypothalamic arcuate nucleus (ARC) are involved in the control of food intake and metabolic processes. It is assumed that, in addition to leptin, the activity of these neurons is regulated by serotonin and dopamine, but only subtype 2C serotonin receptors (5-HT2C R) was identified earlier on the POMC-neurons. The aim of this work was a comparative study of the localization and number of leptin receptors (LepR), types 1 and 2 dopamine receptors (D1 R, D2 R), 5-HT1B R and 5-HT2C R on the POMC-neurons and the expression of the genes encoding them in the ARC of the normal and diet-induced obese (DIO) rodents and the agouti mice (A y /a) with the melanocortin obesity...
April 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29396609/role-of-adenosine-a-2a-receptors-in-motor-control-relevance-to-parkinson-s-disease-and-dyskinesia
#18
REVIEW
Annalisa Pinna, Marcello Serra, Micaela Morelli, Nicola Simola
Adenosine is an endogenous purine nucleoside that regulates several physiological functions, at the central and peripheral levels. Besides, adenosine has emerged as a major player in the regulation of motor behavior. In fact, adenosine receptors of the A2A subtype are highly enriched in the caudate-putamen, which is richly innervated by dopamine. Moreover, several studies in experimental animals have consistently demonstrated that the pharmacological antagonism of A2A receptors has a facilitatory influence on motor behavior...
February 2, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29392842/activation-of-5-ht7-receptor-by-administration-of-its-selective-agonist-lp-211-modifies-explorative-curiosity-behavior-in-rats-in-two-paradigms-which-differ-in-visuospatial-parameters
#19
Cristiana Carbone, Annalisa Adinolfi, Stefano Cinque, Enza Lacivita, Enrico Alleva, Marcello Leopoldo, Walter Adriani
AIMS: The serotonin 7 receptor (5-HT7R) subtype, coded by Htr7 gene, is broadly expressed in the central nervous system (CNS) with clear involvement in behavioral functions such as learning/memory, regulation of mood, and circadian rhythms. In this study, we assessed effects of 5-HT7R stimulation by administration of its selective agonist, LP-211 (0.25 mg/kg i.p.), in adult Wistar-Han rats. METHODS: We used two different explorative-curiosity tests. Drug was administered either before one side-chamber familiarization (CF/V group) or immediately after it, to act on consolidation of familiarization (V/CF group)...
February 1, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29384698/cross-talk-inhibition-between-5-ht-2b-and-5-ht-7-receptors-in-phrenic-motor-facilitation-via-nadph-oxidase-and-pka
#20
Raphael Rodrigues Perim, Daryl P Fields, Gordon S Mitchell
Intermittent spinal serotonin receptor activation elicits phrenic motor facilitation (pMF), a form of spinal respiratory motor plasticity. Episodic activation of either serotonin type-2 (5-HT2 ) or 7 (5-HT7 ) receptors elicits pMF, although they do so via distinct cellular mechanisms known as the Q (5-HT2 ) and S (5-HT7 ) pathways to pMF. When co-activated, these pathways interact via mutual, cross-talk inhibition. Although we have a rudimentary understanding of mechanisms mediating cross-talk interactions between spinal 5-HT2 subtype-A (5-HT2A ) and 5-HT7 receptor activation, we do not know if similar interactions exist between 5-HT2 subtype-B (5-HT2B ) and 5-HT7 receptors...
January 31, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
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