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Six compounds having structural features in common with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) were synthesized and tested in mice for the ability to produce a prolonged decrease in nigrostriatal dopamine (DA) and DA metabolites. The compounds that were prepared and tested include the ester elimination products of the analgetic drugs(More)
It has been demonstrated that within the series of hydroxylated (7-OH, 9-OH) and non-hydroxylated (N-0498) hexahydronaphthoxazines the 9-OH (N-0500) analogue is a very potent centrally acting DA receptor agonist. In in vitro [3H]DP-5,6-ADTN binding experiments, reflecting D-2 dopaminergic activity, N-0500 was equipotent with apomorphine and RU-29717,(More)
A series of mono- (5 and 7) and dihydroxylated (5,6 and 6,7)N-methyl,N-propargyl-2-aminotetralins were studied with respect to their dopamine agonistic and monoamine oxidase inhibitory activities. MAO inhibition was found to be reduced by hydroxylation of the aromatic ring. Among the hydroxylated compounds the 7-OH analogue was the most potent inhibitor in(More)
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