Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.

摘要: A series of 35 stereochemically well-defined C1-methyl-substituted derivatives the potent dopamine (DA) receptor agonist 5-hydroxy-2-(di-n-propylamino)tetralin (5-OH-DPAT) have been synthesized. The compounds were tested for central DA agonistic and antagonistic activity, by use biochemical behavioral tests in rats. In addition, vivo interactions with 5,6-dihydroxy-2-(di-n-propylamino)tetralin (DiPr-5,6-ADTN). On basis pharmacological activity profiles, active classified into four groups: classical pre- postsynaptic agonists, agonists preferential action at presynaptic receptors, antagonists, antagonists receptors. Results obtained indicate that both 2R 2S enantiomers C5-oxygenated 2-aminotetralins may be able to bind receptors but only antipodes are activate O-Methylation (1S,2R)-2-amino-1-methyltetralin tends increase their whereas decrease size N-substituent(s) from n-propyl ethyl or methyl appears