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Masakatsu Fujinoki, Gen L Takei
Sperm hyperactivation is regulated by hormones present in the oviduct. In hamsters, 5-hydroxytryptamine (5HT) enhances hyperactivation associated with the 5HT2 receptor and 5HT4 receptor, while 17β-estradiol (E2) and γ-aminobutyric acid (GABA) suppress the association of the estrogen receptor and GABAA receptor, respectively. In the present study, we examined the regulatory interactions among 5HT, GABA, and E2 in the regulation of hamster sperm hyperactivation. When sperm were exposed to E2 prior to 5HT exposure, E2 did not affect 5HT-enhanced hyperactivation...
February 16, 2017: Journal of Reproduction and Development
Fan Wang, Kaitlyn Knutson, Constanza Alcaino, David R Linden, Simon J Gibbons, Purna Kashyap, Madhusudan Grover, Richard Oeckler, Philip A Gottlieb, Hui Joyce Li, Andrew B Leiter, Gianrico Farrugia, Arthur Beyder
KEY POINTS: The gastrointestinal epithelial enterochromaffin (EC) cell synthesizes the vast majority of the body's serotonin. As a specialized mechanosensor, the EC cell releases this serotonin in response to mechanical forces. However, the molecular mechanism of EC cell mechanotransduction is unknown. In the present study, we show, for the first time, that the mechanosensitive ion channel Piezo2 is specifically expressed by the human and mouse EC cells. Activation of Piezo2 by mechanical forces results in a characteristic ionic current, the release of serotonin and stimulation of gastrointestinal secretion...
January 1, 2017: Journal of Physiology
Tin Sandar Zaw, Phyu Phyu Khin, Uy Dong Sohn
Amitriptyline, a well-known antidepressant, exerts inhibitory effect on electrically stimulated rat colon smooth muscle contraction. In this study, we investigated the signaling pathway of amitriptyline-induced inhibitory effect. Changes in isometric force of colon muscle were recorded on polygraph, and data were analyzed by measuring the inhibitory extent induced by amitriptyline. Firstly, muscles were contracted by stimulation with electric field stimulation (EFS), and then, amitriptyline was added cumulatively to determine its influence effect on EFS...
September 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
Panayotis K Thanos, Lauren Malave, Foteini Delis, Paul Mangine, Katie Kane, Adam Grunseich, Melissa Vitale, Paul Greengard, Nora D Volkow
Cocaine's enhancement of dopamine signaling is crucial for its rewarding effects but its serotonergic effects are also relevant. Here we examined the role of the protein p11, which recruits serotonin 5HT1B and 5HT4 receptors to the cell surface, in cocaine reward. For this purpose we tested wild-type (WT) and p11 knockout (KO) male and female mice for cocaine conditioned place preference (CPP) and its cocaine-induced reinstatement at different abstinence times, after 8 days of extinction and 28 days of being home-caged...
July 2016: Synapse
Ronald Scott Obach, Erik A LaChapelle, Michael A Brodney, Michelle Vanase-Frawley, Gregory W Kauffman, Aarti Sawant-Basak
1.The first generation 5HT-4 partial agonist, 4-{4-[4-Tetrahydrofuran-3-yloxy)-benzo[d]isoxazol-3-yloxymethyl]-piperidin-1-ylmethyl}-tetrahydropyran-4-ol, PF-4995274 (TBPT), was metabolized to N-dealkylated (M1) and an unusual, cyclized oxazolidine (M2) metabolites. M1 and M2 demonstrated pharmacological activity at 5HT receptor subtypes warranting further investigation into their dispositional properties in humans; M2 was a minor component in vitro but was the pre-dominant metabolite identified in human plasma...
December 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Mohammad Nasehi
INTRODUCTION: The plethora of studies indicated that there is a cross talk relationship between harmaline and serotonergic (5-HT) system on cognitive and non-cognitive behaviors. Thus, the purpose of this study is to assess the effects of hippocampal 5-HT4 receptor on memory acquisition deficit induced by harmaline. METHODS: Harmaline was injected peritoneally, while 5-HT4 receptor agonist (RS67333) and antagonist (RS23597-190) were injected intra-hippocampal. A single-trial step-down passive avoidance, open field and tail flick tasks were used for measurement of memory, locomotor activity and pain responses, respectively...
July 2015: Basic and Clinical Neuroscience
D Gallego, O Ortega, C Arenas, I López, E Mans, P Clavé
BACKGROUND: Levosulpiride is a 5HT4 agonist/D2 antagonist prokinetic agent used to improve gastric emptying in patients with functional dyspepsia or gastroparesis. The aim of this study was to characterize its effect on the main in vitro motility patterns in the human fundus, antrum, and jejunum. METHODS: Circular muscle strips from human stomach (antrum and fundus) and jejunum, obtained from 46 patients undergoing bariatric surgery, were studied using organ baths...
June 2016: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
O A Lyubashina, I I Busygina, S S Panteleev, A D Nozdrachev
No abstract text is available yet for this article.
2015: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
Mohammad Nasehi, Maryam Tabatabaie, Fatemeh Khakpai, Mohammad-Reza Zarrindast
In this study, the effects of 5-HT4 receptors of the CA1 on MK801-induced amnesia and hyperlocomotion were examined. One-trial step-down method was used to assess memory retention and then, the hole-board method to assess exploratory behaviors. The results showed that post-training intra-CA1 administration of RS67333 (62.5 and 625 ng/mouse) and RS23597 (1 and 10 ng/mouse) decreased memory consolidation, but it did not alter head-dip counts, head-dip latency and locomotor activity. Similarly, MK801 (0.5 and 1 μg/mouse) decreased memory consolidation, but had no effect on head-dip counts and head-dip latency...
February 5, 2015: Neuroscience Letters
Franco Lapi, Laurent Azoulay, Abbas Kezouh, Jacques Benisty, Ilan Matok, Alessandro Mugelli, Samy Suissa
Serotonin stimulation of the 5HT4 receptor might be responsible for an increased risk of atrial fibrillation (AF). Thus, we assessed whether the use of antidepressants (ADs) is associated with an increased risk of chronic AF (cAF). Using the UK Clinical Practice Research Datalink, a nested case-control analysis was conducted within a cohort of new AD users having a diagnosis of depression and/or anxiety. Cases of cAF occurring during follow-up were individually matched with up to 10 controls on age, sex, year of cohort entry, and duration of follow-up...
April 2015: Journal of Clinical Pharmacology
Talakad G Lohith, Rong Xu, Tetsuya Tsujikawa, Cheryl L Morse, Kacey B Anderson, Robert L Gladding, Sami S Zoghbi, Masahiro Fujita, Robert B Innis, Victor W Pike
The serotonin subtype-4 (5-HT4 ) receptor, which is known to be involved physiologically in learning and memory, and pathologically in Alzheimer's disease, anxiety, and other neuropsychiatric disorders-has few radioligands readily available for imaging in vivo. We have previously reported two novel 5-HT4 receptor radioligands, namely [methoxy-(11) C](1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate; [(11) C]RX-1), and the [(18) F]3-fluoromethoxy analog ([(18) F]RX-2), and in this study we evaluated them by PET in rhesus monkey...
August 4, 2014: Synapse
Shilan Mozaffari, Shekoufeh Nikfar, Mohammad Abdollahi
INTRODUCTION: By targeting different subtypes of 5-hydroxytryptamine (5HT) receptors in the gastrointestinal (GI) tract, several drugs have been introduced for the management of irritable bowel syndrome (IBS). Renzapride is a full agonist for 5HT4 receptor and an antagonist to 5HT2b and 5HT3 receptors which is thought a promising therapeutic agent for constipation predominant IBS (C-IBS) patients due to its accelerating effect on the GI tract. In this meta-analysis, our aim was to evaluate the efficacy and tolerability of renzapride in the management of IBS...
February 24, 2014: Archives of Medical Science: AMS
I N Piyasena, J A Jayasinghe
No abstract text is available yet for this article.
March 2014: Ceylon Medical Journal
Magdy El-Salhy, Tarek Mazzawi, Doris Gundersen, Jan G Hatlebakk, Trygve Hausken
BACKGROUND: Irritable bowel syndrome (IBS) is a common chronic functional gastrointestinal disorder. Post-infectious IBS (PI-IBS) is a subset of IBS that accounts for a large proportion of IBS patients. The PI-IBS symptoms meet the Rome criteria for IBS with diarrhoea (IBS-D) or IBS with mixed bowel habits (IBS-M). A low-grade inflammation has been reported to occur in PI-IBS. Abnormalities in intestinal endocrine cells have been reported in both sporadic IBS and PI-IBS. CASE PRESENTATION: A 20-year-old female with a diagnosis of IBS with constipation (IBS-C), according to Rome III criteria, contracted Campylobacter-induced gastroenteritis, after which her symptom pattern changed to IBS-M...
2013: BMC Research Notes
Agnieszka Pałucha-Poniewiera, Piotr Brański, Joanna M Wierońska, Katarzyna Stachowicz, Anna Sławińska, Andrzej Pilc
RATIONALE: Numerous studies indicate the potential antidepressant actions of several mGlu5 receptor antagonists, including 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine (MTEP). The explanation for the mechanism of these effects might be a key step in finding new antidepressant drugs (AD). OBJECTIVES: The aim of the present study was to investigate the possible role of the serotonergic system in the antidepressant-like activity of MTEP in the tail suspension test (TST) in C57BL/6J mice, using selected antagonists of serotonergic receptors and by applying two different methods of serotonin (5-HT) depletion...
January 2014: Psychopharmacology
L M Kozhevnikova, P V Avdonin
Possible involvement ofcalmodulin in adrenergic and serotoninergic regulation of vascular contractility has been studied. Calmodulin inhibitors trifluoperazine and W-13 suppress vasoconstriction of the rat aorta in response to norepinephrine, serotonin, and serotonin 5HT1A- and 5HT2A-receptor agonists (8-OH-DPAT and DOI, respectively) and do not affect the vasodilatory effect of 5HT1B-, 5HT2B-, and 5HT4-receptors. The force of aorta contraction in response to 8-OH-DPAT increases after the activation of calcium entry through voltage-gated Ca2+-channels...
July 2012: Izvestiia Akademii Nauk. Seriia Biologicheskaia
Koen Schepers, Edward C Hsiao, Trit Garg, Mark J Scott, Emmanuelle Passegué
Adult hematopoiesis occurs primarily in the BM space where hematopoietic cells interact with stromal niche cells. Despite this close association, little is known about the specific roles of osteoblastic lineage cells (OBCs) in maintaining hematopoietic stem cells (HSCs), and how conditions affecting bone formation influence HSC function. Here we use a transgenic mouse model with the ColI(2.3) promoter driving a ligand-independent, constitutively active 5HT4 serotonin receptor (Rs1) to address how the massive increase in trabecular bone formation resulting from increased G(s) signaling in OBCs impacts HSC function and blood production...
October 25, 2012: Blood
Weidong Tong, Yoichi Kamiyama, Tim J Ridolfi, Aaron Zietlow, Jun Zheng, Lauren Kosinski, Kirk Ludwig, Toku Takahashi
BACKGROUND: Clinical studies show that disturbed colonic motility induced by extrinsic nerves damage is restored over time. We studied whether 5-HT3 and 5HT4 receptors are involved in mediating the adaptive mechanisms following parasympathetic denervation. METHODS: Parasympathetic denervation of the entire colon was achieved by bilateral pelvic nerve transection and truncal vagotomy in rats. Colonic transit was measured by calculating the geometric center (GC) of 51Cr distribution...
December 2011: Journal of Surgical Research
Ramin Ataee, Soheila Ajdary, Mehdi Rezayat, Mohammad Ali Shokrgozar, Shadab Shahriari, Mohammad Reza Zarrindast
BACKGROUND: Serotonin (5HT) has been shown to be a mitogenic factor in several carcinomas. Its mitogenic effect is elicited through a wide range of 5HT receptor subtypes. In this study, the effects of 5HT, 5HT3 (1-phenylbiguanide hydrochloride) and 5HT4 (cisapride) agonists in promoting the growth of the HT29 cell line and the growth-inhibition effect of the 5HT3 receptor antagonist (Y-25130 hydrochloride) and 5HT4 receptor antagonist (RS 23597-190) were investigated. The expressions of 5HT3 and 5HT4 receptors in human colon cancer tissues and the HT29 cell line were studied...
March 2010: Archives of Iranian Medicine
L M Kozhevnikova, A G Davydova, P V Avdonin
The goal of this work was to study possible mechanisms underlying the potentiation of vasopressor response to serotonin observed in traumatic shock. Experiments with isolated aorta and mesenteric artery of the rat showed that vasoconstriction is caused by the activation of 5HT2A receptors. Agonists of 5HT1B, 5HT1D, 5HT2B, and 5HT4 receptors induced vasodilation. Agonists of 5HT1A receptors had a dual effect determined by interaction with alpha1-adrenergic receptors and 5HT1A receptors. Plasma membrane depolarization with 15 mM KCl increased the vasoconstrictive force in response to serotonin...
May 2009: Izvestiia Akademii Nauk. Seriia Biologicheskaia
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