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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (3), p.367-370
Hauptverfasser:	LINNANEN, Tero, BRISANDER, Magnus, MOHELL, Nina, JOHANSSON, Anette M
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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