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

T Linnanen; M Brisander; N Mohell; A M Johansson

doi:10.1016/s0960-894x(00)00655-7

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

Bioorg Med Chem Lett. 2001 Feb 12;11(3):367-70. doi: 10.1016/s0960-894x(00)00655-7.

Authors

T Linnanen¹, M Brisander, N Mohell, A M Johansson

Affiliation

¹ Organic Pharmaceutical Chemistry, Uppsala University, Uppsala Biomedical Center, Sweden.

PMID: 11212112
DOI: 10.1016/s0960-894x(00)00655-7

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Aporphines / chemical synthesis
Aporphines / metabolism*
Combinatorial Chemistry Techniques
Dopamine Agonists / chemical synthesis*
Dopamine Agonists / metabolism
Hippocampus / chemistry
Humans
Molecular Conformation
Protein Binding
Receptors, Dopamine D2 / metabolism
Receptors, Serotonin / metabolism
Receptors, Serotonin, 5-HT1
Serotonin Receptor Agonists / chemical synthesis*
Serotonin Receptor Agonists / metabolism
Stereoisomerism
Structure-Activity Relationship

Substances

Aporphines
Dopamine Agonists
Receptors, Dopamine D2
Receptors, Serotonin
Receptors, Serotonin, 5-HT1
Serotonin Receptor Agonists
serotonin 7 receptor
aporphine