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 and 5-HT7 and dopamine D2A receptors.
Linnanen
T
T
Organic Pharmaceutical Chemistry, Uppsala University, Uppsala Biomedical Center, Sweden.
Brisander
M
M
Mohell
N
N
Johansson
A M
AM
D000818:Animals; D001060:Aporphines / Q000138:chemical synthesis / Q000378:metabolism*; D020650:Combinatorial Chemistry Techniques; D018491:Dopamine Agonists / Q000138:chemical synthesis* / Q000378:metabolism; D006624:Hippocampus / Q000737:chemistry; D006801:Humans; D008968:Molecular Conformation; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D001060:Aporphines; D018491:Dopamine Agonists; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists; C104425:serotonin 7 receptor; C081279:aporphine