A Novel Ergot Alkaloid as a 5-HT1A Inhibitor Produced by Dicyma sp.
- 23 October 2003
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 46 (24) , 5117-5120
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 pKi of 10.2 versus the 5-hydroxytryptamine1A receptor subtype. The structure was elucidated by extensive NMR spectroscopy and mass spectrometry.Keywords
This publication has 11 references indexed in Scilit:
- Lysergamides of Isomeric 2,4-Dimethylazetidines Map the Binding Orientation of the Diethylamide Moiety in the Potent Hallucinogenic Agent N,N-Diethyllysergamide (LSD)Journal of Medicinal Chemistry, 2002
- Arylpiperazine Derivatives Acting at 5-HT1A ReceptorsCurrent Medicinal Chemistry, 2002
- Ligands for the investigation of 5-HT autoreceptor functionBrain Research Bulletin, 2001
- Ligand induced conformational states of the 5-HT1A receptorEuropean Journal of Pharmacology, 2001
- 5‐HT1A receptor agonist‐antagonist binding affinity difference as a measure of intrinsic activity in recombinant and native tissue systemsBritish Journal of Pharmacology, 2000
- Functional characterization of the 5-HT terminal autoreceptor in the guinea-pig brain cortexBritish Journal of Pharmacology, 1996
- Nonlinear regression using spreadsheetsTrends in Pharmacological Sciences, 1995
- Identification of Ergobine, a New Natural Peptide Ergot AlkaloidJournal of Natural Products, 1993
- Molecular biology of 5-HT receptorsTrends in Pharmacological Sciences, 1989
- 5-HT and anxiety: Promises and pitfallsPharmacology Biochemistry and Behavior, 1986