Possible biologically active metabolites of 5-hydroxy-6-methyl-2-di-n-propylaminotetralin.

  title={Possible biologically active metabolites of 5-hydroxy-6-methyl-2-di-n-propylaminotetralin.},
  author={Joseph Gerard Cannon and David C. Furlano and D. L. Koble and Jay C. Koons and John Paul Long},
  journal={Life sciences},
  volume={34 17},
4 Citations
Dopamine agonists: structure-activity relationships.
  • J. Cannon
  • Biology, Psychology
    Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques
  • 1985
This review surveys classes of structures for which putative dopaminergic agonism has been reported, and cites structure-activity correlations, and some aspects of metabolism of the agents are addressed, which seem to have relevance to structure- activity considerations and to strategy of drug design.
The Status Quo and the Future
One of the great challenges in dopaminergic structure-activity relationship studies is that the elements of the dopamine molecule can be incorporated within the matrix of a variety of ring systems,


Derivatives of 5-hydroxy-6-methyl-2-aminotetralin.
Three title compounds were designed to provide semirigid congeners of m-tyramine in which the ring position ortho to the phenolic OH is blocked to metabolic hydroxylation and were potent in a cat cardioaccelerator nerve assay, which involves dopamine receptors.
N-Alkylated 2-aminotetralins: central dopamine-receptor stimulating activity.
From the biochemical data it is concluded that an n-propyl group on the nitrogen is optimal for activity, and it is suggested that a possible requirement for a potent agonist is that one of it N substituents must fit into a receptor cavity which, because of its size, can maximally accommodate an n -propyl but also smaller groups like ethyl or methyl.
Enzymatic Oxidation at Carbon
The present chapter will attempt to delineate the current knowledge on mechanism and preferred route of oxidative metabolism at carbon.
Selective reactions using metal phenoxides. Part 1. Reactions with formaldehyde
The reactions between formaldehyde and a series of aryloxymagnesium bromides (1) and their complexes with hexamethylphosphoramide (HMPA) in benzene have been investigated. In the absence of ligand