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Serotonin receptor

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https://www.readbyqxmd.com/read/29150544/estimation-of-circulating-drug-metabolite-exposure-in-human-using-in-vitro-data-and-physiologically-based-pharmacokinetic-modelling-example-of-a-high-metabolite-parent-drug-ratio
#1
R Scott Obach, Jian Lin, Emi Kimoto, Sridhar Duvvuri, Timothy Nicholas, Eugene P Kadar, Larry M Tremaine, Aarti Sawant Basak
TBPT ((R)-4-((4-(((4-((tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol), a serotonin-4 receptor partial agonist, is metabolized to two metabolites: an N-dealkylation product (M1) and a cyclized oxazolidine structure (M2). After administration to humans, the exposure to M1 was low and the exposure to M2 was high, relative to the parent drug, despite this being the opposite in vitro. In this study, projection of the plasma metabolite/parent ratios for M1 and M2 was attempted, using in vitro metabolism, binding, and permeability data in static and dynamic PBPK models...
November 17, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29145495/regulatory-mechanism-of-ccn2-production-by-serotonin-5-ht-via-5-ht2a-and-5-ht2b-receptors-in-chondrocytes
#2
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/29145140/fluoxetine-modulates-the-transcription-of-genes-involved-in-serotonin-dopamine-and-adrenergic-signalling-in-zebrafish-embryos
#3
V Cunha, P Rodrigues, M M Santos, P Moradas-Ferreira, M Ferreira
Neurotransmitters pathways in fish and mammals are phylogenetically conserved. Therefore, the environmental presence of psychopharmaceuticals, such as fluoxetine (FLU), are likely to interact with fish serotonergic, dopaminergic and adrenergic systems, affecting their response and associated biological functions. Hence, the present work aimed at evaluating the effects of FLU in the transcription of genes involved in serotonin, dopamine and adrenergic transporters and receptors signalling in early stages of Danio rerio development...
October 27, 2017: Chemosphere
https://www.readbyqxmd.com/read/29141871/potential-approaches-to-prevent-hypoglycemia-associated-autonomic-failure
#4
REVIEW
Eric Lontchi-Yimagou, Jee Young You, Michelle Carey, Ilan Gabriely, Harry Shamoon, Meredith Hawkins
Clear health benefits are associated with intensive glucose control in type 1 diabetes mellitus (T1DM). However, maintaining near-normal glycemia remains an elusive goal for many patients, in large part owing to the risk of severe hypoglycemia. In fact, recurrent episodes of hypoglycemia lead to 'hypoglycemia-associated autonomic failure' (HAAF), characterized by defective counter-regulatory responses to hypoglycemia. Extensive studies to understand the mechanisms underlying HAAF have revealed multiple potential etiologies, suggesting various approaches to prevent the development of HAAF...
November 14, 2017: Journal of Investigative Medicine: the Official Publication of the American Federation for Clinical Research
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
#5
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/29138116/in-silico-identification-of-genes-involved-in-chronic-metabolic-acidosis
#6
Ishfaq A Sheikh, Adeel Malik, Sameera F M AlBasri, Mohd A Beg
AIMS: Chronic metabolic acidosis (CMA) refers to increased plasma acidity due to disturbed acid-base equilibrium in human body. CMA leads to many dysfunctions including disorders of intestinal metabolism and barrier functions. The human body responds to these intestinal dysfunctions by creating a compensatory mechanism at genomic level in intestinal epithelial cells. This study was to identify the molecular pathways involved in metabolic dysfunction and compensatory adaptations in intestinal epithelium during CMA...
November 11, 2017: Life Sciences
https://www.readbyqxmd.com/read/29136336/effect-of-polymorphisms-on-the-pharmacokinetics-pharmacodynamics-and-safety-of-sertraline-in-healthy-volunteers
#7
Miriam Saiz-Rodríguez, Carmen Belmonte, Manuel Román, Dolores Ochoa, Dora Koller, María Talegón, María C Ovejero-Benito, Rosario López-Rodríguez, Teresa Cabaleiro, Francisco Abad-Santos
Sertraline is a selective serotonin reuptake inhibitor (SSRI) widely metabolized in the liver by cytochrome P450 (CYP) enzymes. Besides, it is a P-glycoprotein substrate. Moreover, serotonin transporters and serotonin receptors are involved in its efficacy and safety. The aim of the present study was to evaluate the role of polymorphisms of metabolizing enzymes, transporters and receptors on the pharmacokinetics, pharmacodynamics and tolerability of sertraline in healthy volunteers. Forty-six healthy volunteers (24 men and 22 women) receiving a 100-mg single oral dose of sertraline were genotyped for 17 genetic variants of CYP enzymes (CYP2B6, CYP2C9, CYP2C19, CYP2D6), ATP binding cassette subfamily B member 1 (ABCB1), Solute carrier family 6 member 4 (SLC6A4), 5-Hydroxytryptamine receptor 2A (HTR2A) and 5-Hydroxytryptamine receptor 2C (HTR2C) genes...
November 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29135714/ritanserin-a-serotonin-2-receptor-antagonist-inhibits-functional-recovery-after-cerebral-infarction
#8
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/29135035/analysis-and-measurement-of-serotonin
#9
REVIEW
András Seitz, Stelvio M Bandiera
Serotonin, also known as 5-hydroxytryptamine, is an important signaling molecule in the central and peripheral nervous systems of humans. Acting through several receptor types, it helps regulate the normal functioning of the gastrointestinal tract, cardiovascular system and brain. Serotonin signaling has also been implicated in the etiology of several diseases, including depression, anxiety disorders, hypertension and irritable bowel syndrome. The present review focuses on the chemical analysis of serotonin in biological fluids and biomatrices and traces the development and application of early methods based on UV absorbance or fluorescence to more widely-used current methods such as high-performance liquid chromatography coupled to mass spectrometry...
November 14, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29134560/neurochemical-and-neurotoxic-effects-of-mdma-ecstasy-and-caffeine-after-chronic-combined-administration-in-mice
#10
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
#11
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/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#12
Theresa Mallick-Searle, Mechele Fillman
PURPOSE: Opioid medications are integral in managing acute moderate-to-severe pain. Opioid analgesics bind to μ (mu), κ (kappa), or δ (delta) opioid receptors in the brain, spinal cord, and digestive tract. However, opioids cause adverse effects that may interfere with their therapeutic use. Some adverse effects wane over time, but patients using opioids for acute pain struggle with opioid-induced nausea and vomiting (OINV) the entire time they take the opioid. This article discusses the underlying mechanisms, clinical implications, and treatment strategies of OINV...
November 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/29130344/neurokinin-1-receptor-antagonists-in-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-focus-on-fosaprepitant
#13
Bernardo L Rapoport, Karin Jordan, Cindy Weinstein
Chemotherapy-induced nausea and vomiting (CINV) remains a challenge in cancer care. Improved understanding of CINV pathophysiology has triggered the development of new antiemetic therapeutic options, such as selective neurokinin-1 (NK1) receptor antagonists (RAs), which effectively prevent CINV when added to a standard antiemetic regimen (serotonin-3 RA and dexamethasone). Aprepitant and its water-soluble prodrug, fosaprepitant dimeglumine, are the most widely used NK1 RAs, with extensive clinical use worldwide...
November 13, 2017: Future Oncology
https://www.readbyqxmd.com/read/29129751/hypoglossal-motoneurons-are-endogenously-activated-by-serotonin-during-the-active-period-of-circadian-cycle
#14
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
#15
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/29128414/mapping-of-the-prenatal-and-postnatal-methamphetamine-effects-on-d1-like-dopamine-m1-and-m2-muscarinic-receptors-in-rat-central-nervous-system
#16
Vladimir Farar, Paulina Valuskova, Maria Sevcikova, Jaromir Myslivecek, Romana Slamberova
Methamphetamine (MA) is worldwide known drug with high potential for addiction that causes dopamine, noradrenaline and serotonin release. MA is also able to increase acetylcholine levels in adult rodents. The aim of this study was to map changes in D1-like dopamine receptors (DR), M1 and M2 muscarinic receptors (MR), and the total number of MR (M1-M5 MR) in the CNS of rats exposed to MA prenatally and in adulthood. Rat mothers were exposed to MA (5mg/kg s.c.) or saline during the entire gestation period and their male offspring were administered in adulthood with single MA (1mg/kg) or saline injection...
November 9, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29128269/post-orgasmic-illness-syndrome-a-review
#17
REVIEW
Hoang Minh Tue Nguyen, Areeg Bala, Andrew T Gabrielson, Wayne J G Hellstrom
INTRODUCTION: Post-orgasmic illness syndrome (POIS) is a rare but debilitating cluster of postejaculatory symptoms affecting men. It is a chronic disorder manifesting as a constellation of flulike and allergic symptoms within seconds, minutes, or hours after ejaculation. POIS can be followed by mental sequelae such as diminished concentration and irritability. POIS negatively affects the life of patients by limiting sexual encounters, dampening romantic prospects, creating internal struggles to avoid eroticism, and affecting patients' schedules...
November 8, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/29127070/an-early-experience-of-mild-adversity-involving-temporary-denial-of-maternal-contact-affects-the-serotonergic-system-of-adult-male-rats-and-leads-to-a-depressive-like-phenotype-and-inability-to-adapt-to-a-chronic-social-stress
#18
Anastasia Diamantopoulou, Theodora Kalpachidou, Georgios Aspiotis, Ioannis Gampierakis, Fotini Stylianopoulou, Antonios Stamatakis
Adverse early life experiences can affect adaptability to chronic stressors and lead to depressive-like behaviors in animal models. We employed an early experience model in which rat pups during postnatal days 10-13 are exposed to a T-maze in which they learn the location of their mother motivated by the rewarding stimulus of maternal contact; one group of rats receives the expected reward, by being allowed contact with the mother upon finding her, while the other group is temporarily denied this contact (Denied Expected Reward, DER), thus experiencing mild adversity...
November 7, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/29126252/monoamines-in-glioblastoma-complex-biology-with-therapeutic-potential
#19
Seamus Patrick Caragher, Robert Raymond Hall, Riasat Ahsan, Atique U Ahmed
Glioblastoma (GBM) is characterized by extremely poor prognoses, despite the use of gross surgical resection, alkylating chemotherapeutic agents, and radiotherapy. Evidence increasingly highlights the role of the tumor microenvironment in enabling this aggressive phenotype. Despite this interest, the role of neurotransmitters, brain-specific messengers underlying synaptic transmission, remains murky. These signaling molecules influence a complex network of molecular pathways and cellular behaviors in many CNS-resident cells including neural stem cells and progenitor cells, neurons, and glia cells...
November 4, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/29125864/psychological-stress-in-aged-female-mice-causes-acute-hypophagia-independent-of-central-serotonin-2c-receptor-activation
#20
Chinami Matsumoto, Chihiro Yamada, Chiharu Sadakane, Miwa Nahata, Tomohisa Hattori, Hiroshi Takeda
Sex differences exist in the activation of the hypothalamic-pituitary-adrenal axis following exposure to stress, and the stress response is further affected by aging. This study was conducted to elucidate the mechanism of hypophagia in aged female mice exposed to stress. Immediately after a stress load, aged female mice exhibited acute hypophagia and a rise in plasma corticosterone levels. The administration of a serotonin 2C receptor (5-HT2CR) antagonist suppressed plasma corticosterone but did not affect the reduction in food intake...
2017: PloS One
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