Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives

Novel rigidified (R)-aporphine derivatives were synthesized from (R)-1,11-carbonylaporphine by ring expansion reactions. The structures of the novel analogues were assigned by NMR spectroscopy and X-ray crystallography. The compounds showed moderate affinities and selectivities at serotonin S-HT1A a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (3), p.367-370
Main Authors: LINNANEN, Tero, BRISANDER, Magnus, MOHELL, Nina, JOHANSSON, Anette M
Format: Article
Language:English
Subjects:
Animals
Aporphines - chemical synthesis
Aporphines - metabolism
Biological and medical sciences
Combinatorial Chemistry Techniques
Dopamine Agonists - chemical synthesis
Dopamine Agonists - metabolism
Hippocampus - chemistry
Humans
Medical sciences
Molecular Conformation
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Protein Binding
Receptors, Dopamine D2 - metabolism
Receptors, Serotonin - metabolism
Receptors, Serotonin, 5-HT1
Serotonin Receptor Agonists - chemical synthesis
Serotonin Receptor Agonists - metabolism
Serotoninergic system
Stereoisomerism
Structure-Activity Relationship
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Summary:Novel rigidified (R)-aporphine derivatives were synthesized from (R)-1,11-carbonylaporphine by ring expansion reactions. The structures of the novel analogues were assigned by NMR spectroscopy and X-ray crystallography. The compounds showed moderate affinities and selectivities at serotonin S-HT1A and 5-HT7 and dopamine D2A receptors.
ISSN:0960-894X
1464-3405
DOI:10.1016/s0960-894x(00)00655-7