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Article
Analysis of the anorectic efficacy of HMR1426 in rodents and its effects on gastric emptying in rats
OBJECTIVES: Pharmacodynamics of HMR1426 in rodents.
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Chapter
Identification of Potassium Channels Associated With H+/K+-Atpase in the Parietal Cell
Gastric H+ secretion via the H+/K+-ATPase is coupled to the uptake of K+. However, the molecular identity of luminal K+ channels enabling K+ recycling in parietal cells was unknown. Cuppoletti and coworkers prese...
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Article
Inhibition of Jurkat-T-lymphocyte Na+/H+-exchanger by CD95(Fas/Apo-1)-receptor stimulation
Mitogenic factors are known to stimulate the Na+/H+-exchanger (NHE), leading to cytosolic alkalinization and/or cell swelling. Conversely, a hallmark of apoptosis is cell shrinkage and CD95-induced apoptosis has...
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Article
Evaluation of a sorbitol dehydrogenase inhibitor on diabetic peripheral nerve metabolism: a prevention study
Aims/hypothesis. Studies of the role of sorbitol dehydrogenase in nerve functional deficits induced by diabetes reported contradictory results. We evaluated whether sorbitol dehydrogenase inhibit...
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Article
KVLQT channels are inhibited by the K+ channel blocker 293B
Previous data have indicated that the chromanol 293B blocks a cAMP activated K+ conductance in the colonic crypt, a K+ conductance in pig cardiac myocytes and the K+ conductance induced by IsK protein expression...
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Article
Inhibition of IKs in guinea pig cardiac myocytes and guinea pig IsK channels by the chromanol 293B
The chromanol derivative 293B was previously shown to inhibit a cAMP regulated K+ conductance in rat colon crypts. Subsequent studies on cloned K+ channels from the rat demonstrated that 293B blocks specifically ...
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Article
A new class of inhibitors of cAMP-mediated Cl− secretion in rabbit colon, acting by the reduction of cAMP-activated K+ conductance
Previously we have shown that arylamino-benzoates like 5-nitro-2-(3-phenylpropylamino)-benzoate (NPPB), which are very potent inhibitors of NaCl absorption in the thick ascending limb of the loop of Henle, are...
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Chapter
Discovery and Development of Diuretic Agents
The history of diuretics goes back a long way. It is believed that paleolithic man discovered the caffeine-containing plants. Beverages containing caffeine were prepared from the seeds and bark of different pl...
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Article
Cell shrinkage stimulates bradykinin-induced cell membrane potential oscillations in NIH 3T3 fibroblasts expressing the ras-oncogene
In NIH 3T3 fibroblasts expressing the Ha-ras oncogene (+ras) bradykinin leads to sustained oscillations of cell membrane potential due to oscillations of intracellular Ca2+ with subsequent activation of Ca2+-sens...
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Chapter
Inhibitors of Nonselective Cation Channels in Cells of the Blood-Brain Barrier
In the antiluminal membrane of isolated capillaries of rat and porcine brain (blood-brain barrier) nonselective cation channels with g = 31 pS were observed in cell-excised membrane patches. The channel inacti...
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Article
Effects of arylaminobenzoate-type chloride channel blockers on equivalent short-circuit current in rabbit colon
Arylaminobenzoates were examined in rabbit colon mounted in an Ussing chamber. The open-circuit transepithelial voltage (V te) and resistance (R te) were measured and the equivalent short-circuit current (I SC=V
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Article
Different types of blockers of the intermediate-conductance outwardly rectifying chloride channel in epithelia
Epithelial chloride channels can be blocked by various inhibitors, which show considerable differences in their molecular structure. In the present patch-clamp study, we compared different blockers of one type...
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Chapter
The Mode of Action of Diuretics
This review will address several recent findings regarding the interaction of so called loop diuretics of the furosemide type with the Na+2Cl−K+ cotransporter in the thick ascending limb of the loop of Henle (TAL...
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Article
Abstract of the 68th Meeting (Spring Meeting) 6–9 March 1990, Heidelberg
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Article
Piretanide-dextran and piretanide-polyethylene glycol interact with high affinity with the Na+ 2 Cl− K+ cotransporter in the thick ascending limb of the loop of Henle
Piretanide blocks the Na+ 2Cl− K+ cotransporter protein in the thick ascending limb (TAL) of the loop of Henle reversibly. When tested from the luminal side in isolated perfused cTAL segments it leads to a half m...
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Article
Characterization of human sweat duct chloride conductance by chloride channel blockers
To characterize the chloride conductance of human sweat duct the effect of various analogues of diphenylamine-2-carboxylate was investigated on the transepithelial potential difference (PDT) and resistance (R ...
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Chapter
Blockers of Active Transport in the Thick Ascending Limb of the Loop of Henle
Loop diuretics of the furosemide type are well known blockers of active NaCl reabsorption in the medullary and in the cortical thick ascending limb of the loop of Henle (1). They interact with one of the Cl- bind...
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Article
Cl−-channel blockers in the thick ascending limb of the loop of Henle Structure activity relationship
On the basis of our findings with diphenylamine-2-carboxylate [5] we have searched for compounds which possess an even higher affinity for the Cl−-channels in the basolateral membrane of the thick ascending limb ...
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Article
Contraluminal sulfate transport in the proximal tubule of the rat kidney
In order to evaluate the specificity for the contraluminal sulfate transport system the inhibitory potency of phenol- and sulfonphthaleins, of sulfamoyl-compounds (diuretics) as well as diphenylamine-2-carboxy...
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Article
Diphenylamine-2-carboxylate, a blocker of the Cl−-conductive pathway in Cl−-transporting epithelia
The present study examines the effects of diphenylamine-2-carboxylate (DPC) in Cl−-transporting epithelia. This substance blocks reversibly the Cl−-conductance present under normal circumstances in the basolatera...
