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calmodulin/diarrhée
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Novel calmodulin antagonist CGS 9343B inhibits secretory diarrhea.
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The goal of this study was to determine whether secretory diarrhea could be ameliorated by pharmacological alteration of the second messenger systems which mediate intestinal fluid and electrolyte transport. Calmodulin is an important intermediate in the mucosal signal-transduction pathways that
Effects of KW-5617 (zaldaride maleate), a potent and selective calmodulin inhibitor, on secretory diarrhea and on gastrointestinal propulsion in rats.
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KW-5617 (zaldaride maleate), 1,3-dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]-benzoxazepin -4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-one maleate, is a selective calmodulin inhibitor. We studied the effects of KW-5617 on secretory diarrhea and gastrointestinal propulsion in rats, as
Zaldaride maleate, an intestinal calmodulin inhibitor, in the therapy of travelers' diarrhea.
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BACKGROUND
The therapeutic value of zaldaride maleate (Zm), an intestinal calmodulin inhibitor, was examined in patients with travelers' diarrhea, known to be caused by enterotoxigenic Escherichia coli (ETEC) and other bacterial agents.
METHODS
One hundred seventy-six American students acquiring
Zaldaride maleate (a new calmodulin antagonist) versus loperamide in the treatment of traveler's diarrhea: randomized, placebo-controlled trial.
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The present study was undertaken to compare the efficacy of a new calmodulin antagonist, zaldaride maleate, with that of placebo or loperamide in persons with traveler's diarrhea. One hundred seventy-nine patients were randomized to receive loperamide (4 mg followed by 2 mg after each unformed
Relationship between anti-diarrheal activity and binding to calmodulin.
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Several neuroleptics known to bind to calmodulin were tested for anti-diarrheal activity and were compared with the opiate anti-diarrheals loperamide and diphenoxylate. All inhibited the intestinal fluid secretion induced by 16,16-dimethyl prostaglandin E2 and castor oil-induced diarrhea in rats as
Pathogenesis and pharmacology of diarrhea.
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The etiological factors involved in diarrhea are multiple. Also the mechanisms and mediators involved are multiple: intracellular mediators (Ca, cAMP, cGMP, calmodulin, phospholipids), extracellular mediators (hormones, neurotransmitters, prostaglandins, enterotoxins...), intramural blood flow and
Travelers' diarrhea. Epidemiology, prevention, and self-treatment.
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Risk factors for travelers' diarrhea include adventurous behavior, consumption of unclean water or food, and special hosts like those taking long acting H2 blockers. Approaches to prevention include education about risk factors, which often fails to lead to modification of risky behavior, and
Magnolol and honokiol regulate the calcium-activated potassium channels signaling pathway in Enterotoxigenic Escherichia coli-induced diarrhea mice.
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To explore the regulatory mechanisms of magnolol and honokiol on calcium-activated potassium channels signaling pathway in Enterotoxigenic Escherichia coli (ETEC)-induced diarrhea mice, the concentrations of serum chloride ion (Cl(-)), sodium ion (Na(+)), potassium ion (K(+)) and calcium ion
A Drosophila Model for Clostridium difficile Toxin CDT Reveals Interactions with Multiple Effector Pathways.
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Clostridium difficile infections (CDIs) cause severe and occasionally life-threatening diarrhea. Hyper-virulent strains produce CDT, a toxin that ADP-ribosylates actin monomers and inhibits actin polymerization. We created transgenic Drosophila lines expressing the catalytic subunit CDTa to
Human rotavirus strain Wa downregulates NHE1 and NHE6 expressions in rotavirus-infected Caco-2 cells.
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Rotavirus (RV) is the most common cause of severe gastroenteritis and fatal dehydration in human infants and neonates of different species. However, the pathogenesis of rotavirus-induced diarrhea is poorly understood. Secretory diarrhea caused by rotavirus may lead to a combination of excessive
[Antidiarrheal agents: tools and therapeutic agents].
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A host of chemically diverse compounds have antidiarrheal potency, however, only a fraction of these agents has gained clinical acceptance. But regardless of their therapeutic status, the effects of these drugs have enhanced our understanding of the physiology and pathophysiology of the intestinal
Comparison of the antidiarrheal effects of zaldaride maleate and its optical isomers in rats.
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Zaldaride maleate (ZAL), a calmodulin inhibitor, that ameliorates secretory diarrhea in rodents, has a racemic structure. In this study, we compared the antidiarrheal and antisecretory effects of ZAL and its optical isomers, R(-)-isomer and S(+)-isomer, in rats. In Ussing chamber experiments, the
Gender differences in the antidiarrheal effect of zaldaride maleate in rats.
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The amelioration of secretory diarrhea has been reported after the administration of zaldaride maleate (ZAL), a selective calmodulin inhibitor, to male rodents. In this study, the antidiarrheal effect of ZAL in female rats was compared with that in male rats. In female and male rats, ZAL
Pharmacological and computational evaluation of Sapodilla and its constituents for therapeutic potential in hyperactive gastrointestinal disorders.
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Objectives
This study was designed to investigate various gastrointestinal effects of Manilkara zapota (Sapodilla), exploring its anti-diarrheal, anti-secretary, anti-spasmodic, anti-ulcer and anti-motility potential.Materials and
Berberine Depresses Contraction of Smooth Muscle via Inhibiting Myosin Light-chain Kinase.
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BACKGROUND
Berberine is a natural isoquinoline alkaloid possessing various pharmacological effects, particularly apparent in the treatment of diarrhea, but the underlying mechanism remains unclear. Smooth muscle myosin light-chain kinase (MLCK) plays a crucial role in the smooth muscle
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