Search Results - "AKUZAWA, Shinobu"
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Effect of ASP8062 on morphine self-administration and morphine-induced respiratory suppression in monkeys
Published in Journal of pharmacological sciences (01-04-2023)“…ASP8062 is an orally available GABAB receptor positive allosteric modulator (PAM). This study assessed the potential of ASP8062 for treating opioid use…”
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Synthesis and structure–activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists
Published in Bioorganic & medicinal chemistry (15-12-2013)“…A series of carbonyl guanidine derivatives have been discovered as potent dual 5-HT2B and 5-HT7 receptor antagonists…”
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Synthesis and structure–activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2
Published in Bioorganic & medicinal chemistry (01-08-2014)“…[Display omitted] We previously reported that the novel dual 5-HT2B and 5-HT7 receptor antagonist N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (4) exerted a…”
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Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists
Published in Bioorganic & medicinal chemistry (01-11-2014)“…[Display omitted] A series of 9-disubstituted N-(9H-fluorene-2-carbonyl)guanidine derivatives have been discovered as potent and orally active dual 5-HT2B and…”
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Evaluation of the Pharmacological Profile of Ramosetron, a Novel Therapeutic Agent for Irritable Bowel Syndrome
Published in Journal of Pharmacological Sciences (2007)“…We examined the pharmacological profile of ramosetron, a 5-HT3-receptor antagonist for irritable bowel syndrome with diarrhea, comparing it with those of other…”
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Effect of ramosetron on conditioned emotional stress-induced colonic dysfunction as a model of irritable bowel syndrome in rats
Published in European journal of pharmacology (14-11-2007)“…The aim of this study was to establish a pathophysiologic model of irritable bowel syndrome, and then to evaluate the pharmaceutical efficacy of ramosetron, a…”
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Inhibitory Effects of Ramosetron, a Potent and Selective 5-HT3–Receptor Antagonist, on Conditioned Fear Stress–Induced Abnormal Defecation and Normal Defecation in Rats: Comparative Studies With Antidiarrheal and Spasmolytic Agents
Published in Journal of Pharmacological Sciences (2008)“…We examined the effect of ramosetron, a potent serotonin (5-HT)3-receptor antagonist for irritable bowel syndrome with diarrhea, on conditioned fear stress…”
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Effects of serotonin 5-HT3 receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats
Published in European journal of pharmacology (10-06-2008)Get full text
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A novel GABAB receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia
Published in European journal of pharmacology (15-12-2019)“…The gamma-aminobutyric acid type B (GABAB) receptor agonist, the sodium salt of gamma-hydroxybutyrate (GHB), significantly improved pain, sleep disturbance and…”
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Effect of antiemetics on zolbetuximab-induced gastric injury and emesis in ferrets
Published in Journal of pharmacological sciences (01-11-2024)“…Claudin-18 splice variant 2 (CLDN18.2), a tight junction protein, is a highly cell type–specific antigen that is expressed by differentiated gastric mucosa…”
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New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT3) receptor agonists for the treatment of constipation
Published in Bioorganic & medicinal chemistry (03-04-2003)“…The syntheses and biological evaluation of a series of novel indeno[1,2-d]thiazole derivatives are described. Several groups reported 5-HT(3) receptor agonists…”
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116.1 GABA-B Agonist Baclofen Normalizes Auditory-Evoked Neural Oscillations and Some Cognitive Deficits in a Fragile X Syndrome Mouse Model
Published in Schizophrenia bulletin (01-03-2017)“…Background: Fragile X syndrome (FXS) is a genetic condition which results from FMR1 gene mutation and leads to intellectual disability, autism-like symptoms…”
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Characterization of [3H]YM060, a potent and selective 5-HT3 receptor radioligand, in the cerebral cortex of rats
Published in European journal of pharmacology (25-07-1995)“…The binding properties of a new radioligand, [methyl-3H]-(-)-(R)-5-[(1-methyl-1H-indol-3-yl)carbonyl]-4,5,6,7- tetrahydro-1H-benzimidazole monohydrochloride…”
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Comparison of [3H]YM060 binding to native and cloned rat 5-HT3 receptors
Published in European journal of pharmacology (25-01-1996)“…We characterized [3H]YM060 ([methyl-3H]-(-)-(R)-5-[(methyl-1H- indol-3-yl)carbonyl]-4,5,6,7-tetrahydro-1H-benzimidazole monohydrochloride) binding in membrane…”
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A novel GABA B receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia
Published in European journal of pharmacology (15-12-2019)“…The gamma-aminobutyric acid type B (GABA ) receptor agonist, the sodium salt of gamma-hydroxybutyrate (GHB), significantly improved pain, sleep disturbance and…”
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Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT sub(2B) and 5-HT sub(7) receptor antagonists
Published in Bioorganic & medicinal chemistry (01-11-2014)“…A series of 9-disubstituted N-(9H-fluorene-2-carbonyl)guanidine derivatives have been discovered as potent and orally active dual 5-HT sub(2B) and 5-HT sub(7)…”
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Biological Activity of Analogues of YM022. Novel (3-Amino Substituted Phenyl)urea Derivatives of 1, 4-Benzodiazepin-2-one as Gastrin : Cholecystokinin-B Receptor Antagonists
Published in Chemical & pharmaceutical bulletin (01-07-1996)“…A series of (3-substituted phenyl)urea analogues of the potent gastrin/cholecystokinin (CCK)-B receptor antagonist YM022 has been prepared. Structure-activity…”
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Hepatic accumulation and hepatotoxicity of luteoskyrin in mice
Published in Toxicology letters (01-06-1992)“…HPLC analysis revealed that luteoskyrin administered orally to male mice accumulated selectively in the liver, with minor distribution to the serum and…”
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Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats
Published in European journal of pharmacology (10-06-2008)“…The effects of corticotropin releasing factor (CRF) and serotonin (5-HT)(3) receptor antagonists on intestinal water transport are not well understood. Hence,…”
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