A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
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.
Vázquez
María J
MJ
Assay Development and Compound Profiling, GlaxoSmithKline R&D, Madrid, Spain. maria-jesus.vazquez@gsk.com
Roa
Ana M
AM
Reyes
Fernando
F
Vega
Alfonso
A
Rivera-Sagredo
Alfonso
A
Thomas
David R
DR
Díez
Emilio
E
Hueso-Rodríguez
Juan A
JA
D000818:Animals; D001203:Ascomycota / Q000737:chemistry*; D001921:Brain / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004873:Ergolines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004876:Ergot Alkaloids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D011869:Radioligand Assay; D044282:Receptor, Serotonin, 5-HT1A / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
D004873:Ergolines; D004876:Ergot Alkaloids; C479888:N-(8'-hydroxy-2'-methyl-5'-(2-methylpropyl)-3',6'-dioxo-7'-(phenylmethyl)oxazolidino(2,3-c)piperazin-2'-yl) 6-methylergoline-8-carboxamide; D012702:Serotonin Antagonists; D044282:Receptor, Serotonin, 5-HT1A; D016244:Guanosine 5'-O-(3-Thiotriphosphate)