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5 HT receptors

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https://www.readbyqxmd.com/read/29145495/regulatory-mechanism-of-ccn2-production-by-serotonin-5-ht-via-5-ht2a-and-5-ht2b-receptors-in-chondrocytes
#1
Ayaka Hori, Takashi Nishida, Shogo Takashiba, Satoshi Kubota, Masaharu Takigawa
Serotonin (5-hydroxytryptamine: 5-HT) is recognized as a neurotransmitter in the central nerve system and as a regulator of systemic blood pressure in the peripheral tissues. Recently, it was reported that 5-HT2 receptors (5-HT2Rs) were expressed in cartilage tissues lacking both vessels and neurons, suggesting possible novel functions of 5-HT during cartilage development and regeneration. Our previous data indicated that CCN family protein 2/connective tissue growth factor (CCN2/CTGF) plays a central role in cartilage development and regeneration...
2017: PloS One
https://www.readbyqxmd.com/read/29143869/peripheral-endocannabinoid-concentrations-are-not-associated-with-verbal-memory-impairment-during-mdma-intoxication
#2
E Haijen, M Farre, R de la Torre, A Pastor, E Olesti, N Pizarro, J G Ramaekers, K P C Kuypers
BACKGROUND: Preclinical data have suggested involvement of the endocannabinoid (eCB) system in MDMA-induced memory impairment. Clinical research has shown that blockade of the 5-HT2 receptor nulls memory impairment during MDMA intoxication. Interestingly, studies have demonstrated that the eCB and the 5-HT system interact. It was hypothesized that MDMA would cause an increase in eCB concentrations together with a decrease in memory performance, and that combining MDMA with a 5-HT2 receptor blocker ketanserin would lead to a counteraction of the MDMA effects on eCB concentrations and memory...
November 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29141182/optogenetic-activation-of-5-ht-neurons-in-the-dorsal-raphe-suppresses-seizure-induced-respiratory-arrest-and-produces-anticonvulsant-effect-in-the-dba-1-mouse-sudep-model
#3
Honghai Zhang, Haiting Zhao, Chang Zeng, Christa Van Dort, Carl L Faingold, Norman E Taylor, Ken Solt, Hua-Jun Feng
Sudden unexpected death in epilepsy (SUDEP) is a devastating epilepsy complication. Seizure-induced respiratory arrest (S-IRA) occurs in many witnessed SUDEP patients and animal models as an initiating event leading to death. Thus, understanding the mechanisms underlying S-IRA will advance the development of preventive strategies against SUDEP. Serotonin (5-HT) is an important modulator for many vital functions, including respiration and arousal, and a deficiency of 5-HT signaling is strongly implicated in S-IRA in animal models, including the DBA/1 mouse...
November 12, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/29139561/the-novel-potent-and-highly-selective-5-ht4-receptor-agonist-yh12852-significantly-improves-both-upper-and-lower-gastrointestinal-motility
#4
Eun Jeong Jeong, Soo Yong Chung, Han Na Hong, Se-Woong Oh, Jae Young Sim
BACKGROUND AND PURPOSE: 5-HT4 receptor agonists have been shown to be effective to treat various gastrointestinal tract disorders. However, a lack of selectivity against off-targets has been a limiting factor. EXPERIMENTAL APPROACH: The binding affinity and selectivity of YH12852 for human 5-HT4(a) receptor in CHO-K1 cells were evaluated using radioligand binding assays, and agonistic activity was assessed using a beta-lactamase reporter system. Contractile activity and propulsive motility were measured in isolated guinea pig distal colon...
November 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29139255/-association-rules-analysis-for-exploring-combined-medication-characteristics-of-fufang-kushen-injection-real-world-study-based-on-49-597-cases
#5
Yin Zhang, Yan-Ming Xie, Yan-Nan Li, Chang Zhang, Cen Chen, Yan Zhuang
The present study aimed to analyze the association rules of Fufang Kushen injection in combined medications in the real world based on electrical medical records in hospital information system, and provide reference for its reasonable clinical application. The electrical medical records of the hospitalized patients using Fufang Kushen injection were extracted to analyze the frequency distribution characteristics in combined application with Western medicine, and analyze the specific association rules between these combinations by using Apriori algorithm...
August 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29138029/synthesis-and-antidepressant-activity-of-a-series-of-arylalkanol-and-aralkyl-piperazine-derivatives-targeting-ssri-5-ht1a-5-ht7
#6
Zheng-Song Gu, Ying Xiao, Qing-Wei Zhang, Jian-Qi Li
A series of arylalkanol and aralkyl piperazine derivatives have been synthesized and evaluated for 5-HT reuptake inhibitory abilities and binding affinities at the 5-HT1A/5-HT7 receptors. Antidepressant activities of the compounds in vivo were screened using the forced swimming test (FST). The results indicated that the compound 8j exhibited high affinities for the 5-HT1A/5-HT7 receptors (5-HT1A, ki = 0.84 nM; 5-HT7, ki = 12 nM) coupling with moderate 5-HT reuptake inhibitory activity (RUI, IC50 = 100 nM) and showed a marked antidepressant-like activity in the FST model...
November 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29135714/ritanserin-a-serotonin-2-receptor-antagonist-inhibits-functional-recovery-after-cerebral-infarction
#7
Kenmei Mizutani, Shigeru Sonoda, Hideaki Wakita
It has been suggested that serotonin (5-HT) may be implicated in functional recovery after stroke; however, the underlying molecular mechanisms remain unknown. Here, the role of 5-HT was verified using ritanserin, a potent 5-HT2A receptor antagonist, and protein expression and modification were analyzed to further understand the association between paralysis recovery and molecular mechanisms in the brain. Experimental cerebral cortex infarctions were induced by photothrombosis in rats. Voluntary exercise was initiated 2 days after surgery...
November 10, 2017: Neuroreport
https://www.readbyqxmd.com/read/29134560/neurochemical-and-neurotoxic-effects-of-mdma-ecstasy-and-caffeine-after-chronic-combined-administration-in-mice
#8
Anna Maria Górska, Katarzyna Kamińska, Agnieszka Wawrzczak-Bargieła, Giulia Costa, Micaela Morelli, Ryszard Przewłocki, Grzegorz Kreiner, Krystyna Gołembiowska
MDMA (3,4-methylenedioxymethamphetamine) is a psychostimulant popular as a recreational drug because of its effect on mood and social interactions. MDMA acts at dopamine (DA) transporter (DAT) and serotonin (5-HT) transporter (SERT) and is known to induce damage of dopamine and serotonin neurons. MDMA is often ingested with caffeine. Caffeine as a non-selective adenosine A1/A2A receptor antagonist affects dopaminergic and serotonergic transmissions. The aim of the present study was to determine the changes in DA and 5-HT release in the mouse striatum induced by MDMA and caffeine after their chronic administration...
November 13, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29133842/serotonin-regulates-prostate-growth-through-androgen-receptor-modulation
#9
Emanuel Carvalho-Dias, Alice Miranda, Olga Martinho, Paulo Mota, Ângela Costa, Cristina Nogueira-Silva, Rute S Moura, Natalia Alenina, Michael Bader, Riccardo Autorino, Estêvão Lima, Jorge Correia-Pinto
Aging and testosterone almost inexorably cause benign prostatic hyperplasia (BPH) in Human males. However, etiology of BPH is largely unknown. Serotonin (5-HT) is produced by neuroendocrine prostatic cells and presents in high concentration in normal prostatic transition zone, but its function in prostate physiology is unknown. Previous evidence demonstrated that neuroendocrine cells and 5-HT are decreased in BPH compared to normal prostate. Here, we show that 5-HT is a strong negative regulator of prostate growth...
November 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29130625/comparative-evaluation-of-68-ga-labeled-nodaga-dotaga-and-hbed-cc-conjugated-cngr-peptide-chelates-as-tumor-targeted-molecular-imaging-probes
#10
Drishty Satpati, Rohit Sharma, Haladhar Dev Sarma, Ashutosh Dash
The biological behavior of (68) Ga-based radiopharmaceuticals can be significantly affected by the chelators' attributes (size, charge, lipophilicity). Thus this study aimed at examining the influence of three different chelators, DOTAGA, NODAGA and HBED-CC on the distribution pattern of (68) Ga-labeled NGR peptides targeting CD13 receptors. (68) Ga-DOTAGA-c(NGR), (68) Ga-NODAGA-c(NGR) and (68) Ga-HBED-CC-c(NGR) were observed to be hydrophilic with respective log P values being -3.5±0.2, -3.3±0.08 and -2...
November 11, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29129751/hypoglossal-motoneurons-are-endogenously-activated-by-serotonin-during-the-active-period-of-circadian-cycle
#11
Leszek Kubin, Graziella L Mann
In obstructive sleep apnea patients, contraction of lingual muscles protects the pharyngeal airway from collapse. Hypoglossal (XII) motoneurons innervate the muscles of the tongue and are themselves under wake-related excitatory drives, including that mediated by serotonin (5-HT). Estimates of endogenous 5-HT activation vary among different studies. We tested whether endogenous drive mediated by 5-HT is present in rat XII motoneurons when measured during the active period of the circadian cycle. We monitored sleep-wake states and lingual and nuchal electromyograms (EMGs) while perfusing the XII nucleus with a vehicle or a 5-HT2 receptor antagonist (mianserin, 0...
November 9, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/29128806/emotional-disorders-induced-by-hemopressin-and-rvd-hemopressin-%C3%AE-administration-in-rats
#12
Sheila Leone, Lucia Recinella, Annalisa Chiavaroli, Sara Martinotti, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Szabolcs Dvorácskó, Csaba Tömböly, Luciano De Petrocellis, Michele Vacca, Luigi Brunetti, Giustino Orlando
BACKGROUND: The endocannabinoid (eCB) system plays an important role in regulating emotional disorders, and is involved, directly or indirectly, in psychiatric diseases, such as anxiety and depression. Hemopressin, a hemoglobin α chain-derived peptide, and RVD-hemopressin(α), a N-terminally extended form of hemopressin, act as antagonist/inverse agonist and negative allosteric modulator of the cannabinoid 1 (CB1) receptor, respectively. METHODS: Considering the possible involvement of these peptides on emotional behaviour, the aim of our study was to investigate the behavioural effects of a single intraperitoneal (ip) injection of hemopressin (0...
June 23, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128212/liver-proteomic-analysis-of-postpartum-holstein-cows-exposed-to-heat-stress-or-cooling-conditions-during-the-dry-period
#13
Amy L Skibiel, Maya Zachut, Bruno C do Amaral, Yishai Levin, Geoffrey E Dahl
Heat stress negatively affects cow performance, compromises immune function, and increases susceptibility to metabolic disorders, particularly during the dry period and as cows transition from gestation to lactation. Metabolic adaptations of the liver are critical for successful transition, yet it is unclear how heat stress affects metabolic pathways within the liver at the proteomic level. The objective of this study was to investigate the liver proteome of postpartum cows that were cooled or heat stressed during the dry period to gain insight into how protein expression is altered by prior heat stress and may contribute to performance and disease outcomes...
November 8, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/29123949/targeting-il-5r%C3%AE-with-antibody-conjugates-reveals-a-strategy-for-imaging-and-therapy-for-invasive-bladder-cancer
#14
Michel Paquette, Luis-Guillermo Vilera-Perez, Simon Beaudoin, Nadia Ekindi-Ndongo, Pierre-Luc Boudreaut, Marc-Andre Bonin, Marie-Claude Battista, M'hamed Bentourkia, Angel F Lopez, Roger Lecomte, Eric Marsault, Brigitte Guérin, Robert Sabbagh, Jeffrey V Leyton
Despite the high interest and concern due to an increasing incidence and death rate, patients who develop muscle invasive bladder cancer (MIBC) have few options available. However, the past decade has produced many candidate bladder tumor-specific markers but further development of these markers is still needed for creating effective targeted medications to solve this urgent need. Interleukin-5 receptor α-subunit (IL-5Rα) has recently been reported to be involved in MIBC progression. Thus, we aimed to validate IL-5Rα as a target for antibody-conjugates to better manage patients with MIBC...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/29123483/impact-of-vortioxetine-on-synaptic-integration-in-prefrontal-subcortical-circuits-comparisons-with-escitalopram
#15
Shreaya Chakroborty, Thomas R Geisbush, Elena Dale, Alan L Pehrson, Connie Sánchez, Anthony R West
Prefrontal-subcortical circuits support executive functions which often become dysfunctional in psychiatric disorders. Vortioxetine is a multimodal antidepressant that is currently used in the clinic to treat major depressive disorder. Mechanisms of action of vortioxetine include serotonin (5-HT) transporter blockade, 5-HT1A receptor agonism, 5-HT1B receptor partial agonism, and 5-HT1D, 5-HT3, and 5-HT7 receptor antagonism. Vortioxetine facilitates 5-HT transmission in the medial prefrontal cortex (mPFC), however, the impact of this compound on related prefrontal-subcortical circuits is less clear...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29119704/pharmacokinetics-of-rp5063-following-single-doses-to-normal-healthy-volunteers-and-multiple-doses-over-10-days-to-stable-schizophrenic-patients
#16
Marc Cantillon, Robert Ings, Laxminarayan Bhat
RP5063, a multimodal dopamine (D)-serotonin (5-HT) stabilizer, possesses high affinity for D2/3/4 and 5-HT1A/2A/2B/2C/6/7 receptors and moderate affinity for the serotonin transporter. Two phase I studies characterized the pharmacokinetics of a single dose (10 and 15 mg fasting, 15 mg fed/fasting) in healthy volunteers and multiple doses (10, 20, 50, and 100 mg fed) over 10 days in patients with stable schizophrenia. RP5063 displayed a dose-dependent Cmax at 4 to 6 h, linear dose proportionality for both Cmax and AUC, and a half-life between 40 and 71 h...
November 8, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/29118192/endocannabinoid-mediated-potentiation-of-non-nociceptive-synapses-contributes-to-behavioral-sensitization
#17
Yanqing Wang, Brian D Burrell
Endocannabinoids, such as 2-arachidonoyl glycerol (2-AG) and anandamide, can elicit long-term depression of both excitatory and inhibitory synapses. This latter effect will result in disinhibition and would therefore be expected to produce an increase in neural circuit output. However, there have been no examples directly linking endocannabinoid-mediated disinhibition to a change in a functional neurobehavioral circuit. The present study uses the well-characterized central nervous system (CNS) of the medicinal leech, Hirudo verbana, to examine the functional/behavioral relevance of endocannabinoid modulation of an identified afferent synapse...
November 8, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/29116249/serotonin-drives-the-acquisition-of-a-profibrotic-and-anti-inflammatory-gene-profile-through-the-5-ht7r-pka-signaling-axis
#18
Ángeles Domínguez-Soto, Alicia Usategui, Mateo de Las Casas-Engel, Miriam Simón-Fuentes, Concha Nieto, Víctor D Cuevas, Miguel A Vega, José Luis Pablos, Ángel L Corbí
Peripheral serotonin (5-hydroxytryptamine, 5-HT) regulates cell growth and differentiation in numerous cell types through engagement of seven types of cell surface receptors (HTR1-7). Deregulated 5-HT/HTR levels contribute to pathology in chronic inflammatory diseases, with macrophages being relevant targets for the physio-pathological effects of 5-HT. In fact, 5-HT skews human macrophage polarization through engagement of 5-HT2BR and 5-HT7R receptors. We now report that 5-HT primes macrophages for reduced pro-inflammatory cytokine production and IFN type I-mediated signaling, and promotes an anti-inflammatory and pro-fibrotic gene signature in human macrophages...
November 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29113874/effect-of-single-doses-of-pindolol-and-d-fenfluramine-on-flumazenil-induced-anxiety-in-panic-disorder-patients
#19
M Bernik, R T Ramos, L A B Hetem, F Graeff
The effects of the 5-HT1A receptor blocker pindolol and the 5-HT releasing and uptake blocking agent d-fenfluramine, both used as indirect serotonin agonists, on flumazenil-induced acute anxiety reactions were studied in panic disorder patients to test the hypothesis that serotonin (5-HT) inhibits neural systems mediating panic attacks. Thirty never treated or drug free PD patients (16 females) aged 22-49 y (mean±SD, 32.9±8) received single doses of d-fenfluramine (n=10; 30mg, p.o.), pindolol (n=10; 5mg, p...
November 4, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29111677/novel-bivalent-5-ht2a-receptor-antagonists-exhibit-high-affinity-and-potency-in-vitro-and-efficacy-in-vivo
#20
Claudia A Soto, Matthew J Shashack, Robert G Fox, Marcy J Bubar, Kenner C Rice, Cheryl S Watson, Kathryn A Cunningham, Scott R Gilbertson, Noelle C Anastasio
The 5-HT2AR plays an important role in various neuropsychiatric disorders including cocaine use disorder and schizophrenia. Homodimerization of this receptor has been suggested but tools that allow direct assessment of 5-HT2AR:5-HT2AR homodimer relevance in these disorders are necessary. We chemically modified the selective 5-HT2AR antagonist M100907 to synthesize a series of homobivalent ligands connected by ethylene glycol linkers of varying lengths that may be useful tools to probe 5-HT2AR:5-HT2AR homodimer function...
November 7, 2017: ACS Chemical Neuroscience
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