PREPARATION AND PHARMACOLOGICAL EVALUATION OF ENANTIOMERS OF CERTAIN NONOXYGENATED APORPHINES - (- AND (-)-APORPHINE AND (+)- AND (-)-10-METHYLAPORPHINE())
Jg. Cannon et al., PREPARATION AND PHARMACOLOGICAL EVALUATION OF ENANTIOMERS OF CERTAIN NONOXYGENATED APORPHINES - (- AND (-)-APORPHINE AND (+)- AND (-)-10-METHYLAPORPHINE()), Journal of medicinal chemistry, 36(10), 1993, pp. 1316-1318
The subject compounds were prepared as a part of a continuing structur
e-activity study of the contrasting actions (agonism-antagonism) of ()- and (-)-11-hydroxy-10-methylaporphine at serotonin (5-HT1A) recepto
rs. None of the targeted nonoxygenated aporphine derivatives demonstra
ted significant activity in assays for any effects at serotonin 5-HT1A
receptors. It is concluded that, in the aporphine series, serotonergi
c agonist or antagonism requires an alkyl group ortho to a phenolic OH
group in the A ring.