Abstract
Ro 46-2005 is a new synthetic non-peptide endothelin (ET) receptor antagonist. In binding experiments, Ro 46-2005 proved to be equipotent (IC50 200-500 nM) for inhibition of [125]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Scatchard analysis was consistent with a competitive binding mode. Ro 46-2005 also inhibited the functional consequences of ET-1 stimulation: the ET-1 induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 microM.
MeSH terms
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Animals
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Aorta / metabolism
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Arachidonic Acid / metabolism
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Binding, Competitive
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Cell Line
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Cells, Cultured
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Cerebellum / metabolism
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Endothelin Receptor Antagonists*
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Endothelins / metabolism*
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Female
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Glomerular Mesangium / drug effects
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Glomerular Mesangium / metabolism*
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Humans
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Intracellular Membranes / metabolism
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Kinetics
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Microsomes / metabolism
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Moths
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Muscle, Smooth / metabolism*
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Muscle, Smooth, Vascular / metabolism*
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Placenta / metabolism
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Pregnancy
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Pyrimidines / pharmacology*
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Rats
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Receptors, Endothelin / metabolism*
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / metabolism
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Sulfonamides / pharmacology*
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Swine
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Transfection
Substances
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Endothelin Receptor Antagonists
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Endothelins
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Pyrimidines
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Receptors, Endothelin
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Recombinant Proteins
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Sulfonamides
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Ro 46-2005
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Arachidonic Acid