Abstract
In the course of a search for small-molecule inhibitors of 5-hydroxytryptamine receptors we have identified a novel ergoline derivative (1) from the fungal culture of Dicyma sp. This compound has a pK(i) of 10.2 versus the 5-hydroxytryptamine(1A) receptor subtype. The structure was elucidated by extensive NMR spectroscopy and mass spectrometry.
MeSH terms
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Animals
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Ascomycota / chemistry*
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Brain / drug effects
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Brain / metabolism
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Brain / ultrastructure
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Cell Membrane / drug effects
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Cell Membrane / metabolism
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Ergolines / chemistry
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Ergolines / isolation & purification*
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Ergolines / pharmacology
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Ergot Alkaloids / chemistry
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Ergot Alkaloids / isolation & purification*
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Ergot Alkaloids / pharmacology
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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In Vitro Techniques
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Magnetic Resonance Spectroscopy
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Radioligand Assay
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Receptor, Serotonin, 5-HT1A / drug effects*
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Receptor, Serotonin, 5-HT1A / metabolism
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Serotonin Antagonists / chemistry
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Serotonin Antagonists / isolation & purification*
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Serotonin Antagonists / pharmacology
Substances
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Ergolines
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Ergot Alkaloids
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N-(8'-hydroxy-2'-methyl-5'-(2-methylpropyl)-3',6'-dioxo-7'-(phenylmethyl)oxazolidino(2,3-c)piperazin-2'-yl) 6-methylergoline-8-carboxamide
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Serotonin Antagonists
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Receptor, Serotonin, 5-HT1A
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Guanosine 5'-O-(3-Thiotriphosphate)