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https://www.readbyqxmd.com/read/28090679/effect-of-prucalopride-on-intestinal-gas-tolerance-in-patients-with-functional-bowel-disorders-and-constipation
#1
RANDOMIZED CONTROLLED TRIAL
Carolina Malagelada, Adoración Nieto, Sara Mendez, Anna Accarino, Javier Santos, Juan-R Malagelada, Fernando Azpiroz
BACKGROUND AND AIM: Patients with functional bowel disorders develop gas retention and symptoms in response to intestinal gas loads that are well tolerated by healthy subjects. Stimulation of 5HT-4 receptors in the gut has both prokinetic and antinociceptive effects. The aim of this study is to determine the effect of prucalopride, a highly selective 5HT-4 agonist, on gas transit and tolerance in women with functional bowel disorders complaining of constipation. METHODS: Twenty-four women with functional bowel disorders complaining of constipation were included in the study...
August 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/26947511/strategies-toward-optimization-of-the-metabolism-of-a-series-of-serotonin-4-partial-agonists-investigation-of-azetidines-as-piperidine-isosteres
#2
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
https://www.readbyqxmd.com/read/22888336/does-cisapride-as-a-5ht-4-receptor-agonist-aggravate-the-severity-of-tnbs-induced-colitis-in-rat
#3
Azadeh Motavallian, Mohsen Minaiyan, Mohammad Rabbani, Parvin Mahzouni, Sasan Andalib, Alireza Abed, Mohammad Reza Babavalian
There is a pressing need for research that will lead to the reveal of targets designed to analyse the possible pathways for the treatment of IBD. Because of the probable involvement of serotonin in inflammatory conditions of intestine and the important role of 5HT(4) receptors in GI function, the investigation of the role of 5HT(4) receptors in the pathogenesis of IBD will be interesting. The aim of this study was to investigate the effects of cisapride, a 5HT(4) receptor agonist, in trinitrobenzenesulfonic-acid-(TNBS) induced rat colitis...
2012: Gastroenterology Research and Practice
https://www.readbyqxmd.com/read/22296841/irritable-bowel-syndrome
#4
REVIEW
Alexander Charles Ford, Per Olav Vandvik
INTRODUCTION: The prevalence of irritable bowel syndrome (IBS) varies depending on the criteria used to diagnose it, but it ranges from about 5% to 20%. IBS is associated with abnormal gastrointestinal motor function and enhanced visceral perception, as well as psychosocial and genetic factors. People with IBS often have other bodily and psychiatric symptoms, and have an increased likelihood of having unnecessary surgery compared with people without IBS. METHODS AND OUTCOMES: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments in people with IBS? We searched: Medline, Embase, The Cochrane Library, and other important databases up to August 2011 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review)...
2012: Clinical Evidence
https://www.readbyqxmd.com/read/21718578/irritable-bowel-syndrome
#5
REVIEW
Alexander Charles Ford, Per Olav Vandvik
INTRODUCTION: The prevalence of irritable bowel syndrome (IBS) varies depending on the criteria used to diagnose it, but it ranges from about 5% to 20%. IBS is associated with abnormal gastrointestinal motor function and enhanced visceral perception, as well as psychosocial and genetic factors. People with IBS often have other bodily and psychiatric symptoms, and have an increased likelihood of having unnecessary surgery compared with people without IBS. METHODS AND OUTCOMES: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments in people with IBS? We searched: Medline, Embase, The Cochrane Library, and other important databases up to July 2009 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review)...
2010: Clinical Evidence
https://www.readbyqxmd.com/read/21350320/-guidelines-for-the-treatment-of-irritable-bowel-syndrome
#6
Joong Goo Kwon, Kyung Sik Park, Jung Ho Park, Jae Myung Park, Cheol Hee Park, Kwang Jae Lee, Hyo Jin Park, Jong Chul Rhee
Traditional symptom-based therapies of irritable bowel syndrome (IBS) are directed at the relief of individual IBS symptoms, but they are often of limited efficacy in addressing the entire symptom complex. Combinations of drugs to target bothersome symptoms are suggested as the first-line pharmacologic treatment. Increasing knowledge of the pathophysiology and molecular mechanisms of IBS has resulted in the development of several new therapeutic approaches. Thirteen consensus statements for the treatment of IBS were developed using the modified Delphi approach...
February 2011: Korean Journal of Gastroenterology, Taehan Sohwagi Hakhoe Chi
https://www.readbyqxmd.com/read/20964689/regulation-of-protein-kinase-c-apl-ii-by-serotonin-receptors-in-aplysia
#7
COMPARATIVE STUDY
Ikue Nagakura, Tyler W Dunn, Carole Abi Farah, Andrew Heppner, Flora F Li, Wayne S Sossin
Serotonin (5-hydroxytryptamine, 5HT) is the neurotransmitter that mediates dishabituation in Aplysia. Serotonin mediates this behavioral change through the reversal of synaptic depression in sensory neurons (SNs). However, the 5HT receptors present in SNs and in particular, the receptor important for activation of protein kinase C (PKC) have not been fully identified. Using a recent genome assembly of Aplysia, we identified new receptors from the 5HT(2) , 5HT(4) , and 5HT(7) families. Using RT-PCR from isolated SNs, we found that three 5HT receptors, 5HT(1Apl(a)) , 5HT(2Apl) , and 5HT(7Apl) were expressed in SNs...
November 2010: Journal of Neurochemistry
https://www.readbyqxmd.com/read/20850200/-levosulpiride-in-the-management-of-functional-dyspepsia-and-delayed-gastric-emptying
#8
REVIEW
Jordi Serra
Levosulpiride is a sulpiride isomer that exerts its prokinetic action through a dual mechanism: 1) as a D(2) dopamine receptor antagonist and 2) as a serotonin 5HT(4) receptor agonist, conferring this drug with a cholinergic effect. At a dosage of 25mg three times daily, levosulpiride accelerates gastric and gallbladder emptying. Clinical trials have shown that this agent is more effective than placebo in reducing the symptoms of dyspepsia, while comparative studies have demonstrated that its effect is similar or superior to that of other dopamine antagonists...
October 2010: Gastroenterología y Hepatología
https://www.readbyqxmd.com/read/20711435/update-on-the-management-of-constipation-in-the-elderly-new-treatment-options
#9
REVIEW
Satish S C Rao, Jorge T Go
Constipation disproportionately affects older adults, with a prevalences of 50% in community-dwelling elderly and 74% in nursing-home residents. Loss of mobility, medications, underlying diseases, impaired anorectal sensation, and ignoring calls to defecate are as important as dyssynergic defecation or irritable bowel syndrome in causing constipation. Detailed medical history on medications and co-morbid problems, and meticulous digital rectal examination may help identify causes of constipation. Likewise, blood tests and colonoscopy may identify organic causes such as colon cancer...
August 9, 2010: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/20060191/the-effect-of-mosapride-5ht-4-receptor-agonist-on-insulin-sensitivity-and-glut4-translocation
#10
RANDOMIZED CONTROLLED TRIAL
J S Nam, J Y Nam, J S Yoo, M Cho, J S Park, C W Ahn, B S Cha, E J Lee, S K Lim, K R Kim, H C Lee
AIMS: We investigated the effect of mosapride, 5HT-4 (5-hydroxytryptamine) agonist, on blood glucose level and insulin sensitivity in subjects with impaired glucose tolerance (IGT) and conducted an in vitro study to evaluate the action mechanism. METHODS: Thirty IGT patients were randomly assigned to receive either mosapride or placebo for 2 weeks. Biochemical profiles and insulin sensitivity index from euglycemic hyperinsulinemic clamp test were assessed before and after treatment...
March 2010: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/19751247/safety-assessment-of-prucalopride-in-elderly-patients-with-constipation-a-double-blind-placebo-controlled-study
#11
RANDOMIZED CONTROLLED TRIAL
M Camilleri, G Beyens, R Kerstens, P Robinson, L Vandeplassche
Chronic constipation is common among nursing home residents. The aim of this study was to evaluate safety, tolerability and pharmacokinetics of the selective 5HT(4) receptor agonist prucalopride in elderly, chronically constipated patients in nursing homes. A multicentre, phase II, randomized, double-blind dose-escalation study in 89 elderly constipated nursing home residents treated with placebo, 0.5, 1 or 2 mg prucalopride once daily for 28 days was analysed. Adverse events, vital signs, ECG, Holter monitor and pharmacokinetics were assessed (Clinicaltrials...
December 2009: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/19454062/irritable-bowel-syndrome
#12
REVIEW
Niek de Wit, Gregory Rubin, Roger Hugh Jones
INTRODUCTION: The prevalence of irritable bowel syndrome (IBS) varies depending on the criteria used to diagnose it, but ranges from about 5% to over 15%. IBS is associated with abnormal gastrointestinal motor function and enhanced visceral perception, as well as psychosocial and genetic factors. People with IBS have an increased likelihood of having a cholecystectomy or hysterectomy compared with people without IBS. METHODS AND OUTCOMES: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments in people with IBS? We searched: Medline, Embase, The Cochrane Library and other important databases up to June 2006 (BMJ Clinical evidence reviews are updated periodically, please check our website for the most up-to-date version of this review)...
2007: Clinical Evidence
https://www.readbyqxmd.com/read/18672092/serotonergic-agents-and-the-irritable-bowel-syndrome-what-goes-wrong
#13
REVIEW
Robin Spiller
It is now nine years since the first large randomised controlled trials showed the benefit of a 5HT(3) antagonist in irritable bowel syndrome (IBS) with diarrhoea (IBS-D) and a 5HT(4) partial agonist in IBS with constipation (IBS-C). Although both of these drugs have now been withdrawn because of rare complications (ischaemic colitis and thrombotic episodes respectively), their clinical effectiveness has stimulated substantial advances in our understanding of the physiological role of serotonin and its disturbance in IBS...
December 2008: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/17943807/tegaserod-for-the-treatment-of-irritable-bowel-syndrome-and-chronic-constipation
#14
REVIEW
B W Evans, W K Clark, D J Moore, P J Whorwell
BACKGROUND: IBS is a complex disorder that encompasses a wide profile of symptoms. The symptoms of chronic constipation frequently resemble those of constipation-predominant IBS. Current drug treatments for irritable bowel syndrome (IBS) are of limited value. Many target specific symptoms only. Tegaserod, a 5HT(4) partial agonist, represents a novel mechanism of action in the treatment of IBS and chronic constipation. OBJECTIVES: The objective of this review was to evaluate the efficacy and tolerability of tegaserod for the treatment of IBS and chronic constipation in adults and adolescents aged 12 years and above...
2007: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/17620083/importance-of-5-hydroxytryptamine-receptors-on-intestinal-afferents-in-the-regulation-of-visceral-sensitivity
#15
REVIEW
B Greenwood-van Meerveld
Serotonin (5-HT) plays an important role as a signalling molecule in the gastrointestinal (GI) tract. The regulation of GI sensitivity via 5-HT is mediated by specific 5-HT receptor subytypes on intrinsic and extrinsic afferents. This review discusses visceral afferent hypersensitivity in irritable bowel syndrome (IBS) and the importance of 5HT(3), 5HT(4), and 5HT(2B) receptor-mediated mechanisms in the regulation of visceral sensitivity.
August 2007: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/16469039/the-effect-of-serotonin-and-serotonin-antagonists-on-bladder-cancer-cell-proliferation
#16
Emad J Siddiqui, Majid A Shabbir, Dimitri P Mikhailidis, Faiz H Mumtaz, Cecil S Thompson
OBJECTIVE: To investigate the role of serotonin (5-hydroxytryptamine, 5HT) and its antagonists in the proliferation of high-grade bladder cancer cells (HT1376), as high-grade bladder cancer has a rapid rate of progression, invasion and recurrence, and 5HT antagonists inhibit the growth of the prostate cancer cell line (PC3). MATERIALS AND METHODS: HT1376 (human grade III transitional cell carcinoma) cells were incubated with either 5HT or 5HT antagonists (5HT(1A), 5HT(1B), 5HT(1D), 5HT(2), 5HT(3) and 5HT(4))...
March 2006: BJU International
https://www.readbyqxmd.com/read/16229866/5-hydroxytryptamine-induced-excitation-and-inhibition-in-the-subthalamic-nucleus-action-at-5-ht-2c-5-ht-4-and-5-ht-1a-receptors
#17
I M Stanford, M A Kantaria, H S Chahal, K C Loucif, C L Wilson
Extracellular single-unit recordings in mouse brain slices were used to determine the effect of exogenously applied 5-HT on STN neurones. Recordings were made from 74 STN cells which fired action potentials at a regular rate of 7.19+/-0.5 Hz. In 61 cells (82%), 5-HT application increased STN neurone firing rate (10 microM, 180+/-16.8%, n=35) with an estimated EC(50) of 5.4 microM. The non-specific 5-HT(2) receptor agonist alpha-methyl 5-HT (1-10 microM) mimicked 5-HT induced excitations (15 cells). These excitations were significantly reduced by pre-perfusion with the specific 5-HT(2C) receptor antagonist RS102221 (500 nM, 9 cells) and the 5HT(4) antagonist GR113808 (500 nM, 7 cells)...
December 2005: Neuropharmacology
https://www.readbyqxmd.com/read/15563764/receptor-regulatory-properties-evident-in-the-molecular-similarity-of-serotonin-receptor-ligands-and-purine-nucleotides
#18
W R Williams, W J Pugh, P J Nicholls
Previous computational studies have explored the relative molecular similarity inherent in the ligands of neurotransmitter-regulated cell receptors and purine nucleotides. This study presents the results of an investigation of the major serotonin (5-HT) receptor classes, using molecular superimposition and fitting data. Ligands for 5HT(1B/C/D) and 5HT(4/7) receptors identified pharmacophores in the adenine ring of ATP. 5-HT(2) and 5-HT(3) receptor ligands identified pharmacophores in the guanosine nucleotide and cyclic nucleotide, respectively...
December 2004: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/14974049/tegaserod-for-the-treatment-of-irritable-bowel-syndrome
#19
REVIEW
B W Evans, W K Clark, D J Moore, P J Whorwell
BACKGROUND: IBS is a complex disorder that encompasses a wide profile of symptoms. Current drug treatments for irritable bowel syndrome (IBS) are of limited value. Many target specific symptoms only. Tegaserod, a 5HT(4) partial agonist, represents a novel mechanism of action in the treatment of IBS. OBJECTIVES: The objective of this review was to evaluate the efficacy and tolerability of tegaserod for the treatment of IBS in adults and adolescents aged 12 years and above...
2004: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/12934054/responses-to-serotonin-5ht-in-isolated-corpus-cavernosum-penis-of-rabbit
#20
K Furukawa, K Nagao, N Ishii, T Uchiyama
This study was aimed at determining serotonin (5-hydroxytryptamine: 5HT) receptor subtypes participating in 5HT-induced response in the isolated corpus cavernosum penis (CCP) of rabbits. 5HT contracted the CCP in a concentration-dependent manner. Both WAY100635 (5HT(1A) antagonist) and LY53857 (5HT(2) antagonist) concentration-dependently suppressed the 5HT-induced contraction. The suppression of the 5HT-induced contraction by ketanserin (5HT(2A) antagonist) was weaker than that by LY53857. LY278584 (5HT(3) antagonist) did not affect the 5HT-induced contraction...
August 2003: International Journal of Impotence Research
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