Search Results - "KAMEI, Kenshi"
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An orally active motilin receptor antagonist, MA-2029, inhibits motilin-induced gastrointestinal motility, increase in fundic tone, and diarrhea in conscious dogs without affecting gastric emptying
Published in European journal of pharmacology (01-08-2009)“…The pharmacological properties of MA-2029, a selective and competitive motilin receptor antagonist, were investigated in conscious dogs after oral…”
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Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits
Published in European journal of pharmacology (10-03-2008)“…The pharmacological properties of MA-2029, a novel motilin receptor antagonist, were investigated. In vitro, MA-2029 (1 to 30 nM) competitively inhibited…”
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MITEMCINAL (GM-611), AN ORALLY ACTIVE MOTILIN RECEPTOR AGONIST, IMPROVES DELAYED GASTRIC EMPTYING IN A CANINE MODEL OF DIABETIC GASTROPARESIS
Published in Clinical and experimental pharmacology & physiology (01-07-2008)“…SUMMARY 1 The aim of the present study was to evaluate the effects of mitemcinal (GM‐611), an orally active motilin receptor agonist, on delayed gastric…”
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Effects of mitemcinal (GM-611), an acid-resistant nonpeptide motilin receptor agonist, on the gastrointestinal contractile activity in conscious dogs
Published in Pharmacology (01-01-2007)“…The effects of mitemcinal (GM-611) on the gastrointestinal contractile activity were investigated using chronically implanted force transducers in conscious…”
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ORAL MITEMCINAL (GM-611), AN ERYTHROMYCIN-DERIVED PROKINETIC, ACCELERATES NORMAL AND EXPERIMENTALLY DELAYED GASTRIC EMPTYING IN CONSCIOUS DOGS
Published in Clinical and experimental pharmacology & physiology (01-01-2008)“…SUMMARY 1 We examined effects of orally administered mitemcinal, an erythromycin‐derived motilin agonist, on gastric emptying and antroduodenal motility in…”
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Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics
Published in Bioorganic & medicinal chemistry letters (01-07-2009)“…Peptidomimetic motilin antagonists ( 17c and 17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in…”
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Contractile mechanism of GM-611 on gastrointestinal motility in conscious dogs
Published in Japanese Journal of Pharmacology (2000)“…GM-611, an acid-resistant erythromycin A derivative, is currently under clinical trials as a gastroprokinetic agent. It has been demonstrated that GM-611…”
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Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-Imidazolyl)alkyl]-1(2H)-phthalazinones
Published in Journal of medicinal chemistry (01-12-1993)“…A number of 4-substituted 2-[omega-(1-imidazolyl)alkyl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane A2…”
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Effects of KC-515, a new K channel opener, in several hypertensive and hyperlipidemia models of rats
Published in Japanese Journal of Pharmacology (1994)“…KC-515 is a newly synthesized potent potassium channel opener. We examined antihypertensive effects of KC-515 in several conscious rat models of experimental…”
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Acceleratory effect of GM-611 on defecation in rabbits
Published in Journal of Pharmacological Sciences (2003)“…GM-611, a motilin receptor agonist, is currently under clinical trials as a gastroprokinetic agent. It has been demonstrated that GM-611 stimulates the upper…”
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11
Hemodynamic and Hormonal Responses to Nicorandil in a Canine Model of Acute Ischemic Heart Failure: A Comparison with Cromakalim and Nitroglycerin
Published in Journal of cardiovascular pharmacology (01-01-1999)“…The pharmacologic profiles of nicorandil in the cardiovascular system have been characterized by K-channel opening and nitrate activities. However, the effects…”
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12
Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 2. 4-(3-Pyridyl)-1(2H)-phthalazinones
Published in Journal of medicinal chemistry (01-12-1993)“…A series of novel 4-(3-pyridyl)-1(2H)-phthalazinone derivatives which possess dual activities of thromboxane A2 (TXA2) synthetase inhibition and…”
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13
Regional and species differences in glyburide‐sensitive K+ channels in airway smooth muscles as estimated from actions of KC 128 and levcromakalim
Published in British journal of pharmacology (01-11-1994)“…1 The purpose of the present experiments was to elucidate the differences in actions of two K+ channel openers, KC 128 and levcromakalim, on the…”
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Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. V: Thienopyridazinone derivatives
Published in Chemical & pharmaceutical bulletin (1995)“…Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the…”
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Effect of KC399, a newly synthesized K+ channel opener, on acetylcholine‐induced electrical and mechanical activities in rabbit tracheal smooth muscle
Published in British journal of pharmacology (01-08-1995)“…1 Effects of KC399, an opener of ATP‐sensitive K+ channels were investigated on membrane potential, isometric force and intracellular Ca2+ ([Ca2+]i…”
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Novel Antiasthmatic Agents with Dual Activities of Thromboxane A2 Synthetase Inhibition and Bronchodilation. V.Thienopyridazinone Derivatives
Published in Chemical and Pharmaceutical Bulletin (15-02-1995)“…Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described.A thiophene ring was found to be able to replace the…”
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Novel Antiasthematic Agents with Dual Activities of Thromboxane A2 Synthetase Inhibition and Bronchodilation. IV.2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl-1(2H)-phthalazinones
Published in Chemical & pharmaceutical bulletin (15-09-1994)“…Synthesis and pharmacological evaluation of several compounds related to 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones are described. The phenyl…”
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Novel Antiasthmatic Agents with Dual Activities of Thromboxane A2 Synthetase Inhibition and Bronchodilation. III. 4-[2-(5-Ethyl-2-thienyl)]-2'-[2-(1-imidazolyl)ethyl]-1(2H)-phthalazinones
Published in Chemical & pharmaceutical bulletin (01-08-1994)“…Synthesis and pharmacological evaluation of novel 4-[2-(5-ethyl-2-thienyl)]-2-[2-(1-imidazolyl)ethyl]-1(2H)-phthalazinones are described. The phenyl moiety of…”
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Novel Antiasthmatic Agents with Dual Activities of Thromboxane A2 Synthetase Inhibition and Bronchodilation. VI. Indazole Derivatives
Published in Chemical & pharmaceutical bulletin (1995)“…Synthesis and pharmacological evaluation of novel indazole derivatives are described. These compounds were found to exhibit both thromboxane A2 (TXA2)…”
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Contribution of the tissue angiotensin converting enzyme to the antihypertensive effect of altiopril calcium (MC-838) in spontaneously hypertensive rats
Published in Journal of pharmacy and pharmacology (01-04-1989)“…The effect of a new orally active angiotensin converting enzyme (ACE) inhibitor, calcium (-)-N-[(S)-3-[(N-cyclohexylcarbonyl-D-alanyl)thio]-2-methylpropionyl+…”
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