Structure-activity relationship studies of CNS agents. Part II. De novo analysis of the monoamine uptake inhibition data of 1-alkylamino-4-aryltetralins.
A quantitative structure-activity relationship (QSAR) was analyzed for monoamine uptake inhibition of cis- and trans-1-alkylamino-4-aryltetralins using the Free-Wilson method. The calculated individual substituent contributions were found to be strongly correlated with the uptake inhibition activity of dopamine, 5-hydroxytryptamine and norepinephrine in the corpus striatum and hypothalamus of rats, respectively. The effect of the substituents and stereochemical factors on the monoamine uptake inhibition of the analyzed series of tetralins was discussed.
Mokrosz
J L
JL
Department of Organic Chemistry, Polish Academy of Sciences, Kraków.
D000818:Animals; D015306:Biogenic Monoamines / Q000378:metabolism*; D001921:Brain / Q000378:metabolism*; D014179:Neurotransmitter Uptake Inhibitors / Q000378:metabolism*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000378:metabolism*
D015306:Biogenic Monoamines; D014179:Neurotransmitter Uptake Inhibitors; D013764:Tetrahydronaphthalenes