• Corpus ID: 36131668

The 2-aminotetralin system as a structural base for new dopamine- and melatonin-receptor agents

  title={The 2-aminotetralin system as a structural base for new dopamine- and melatonin-receptor agents},
  author={Swier Copinga},
The research described in this thesis is divided into two parts. Part I (chapters 1-3) deals with the development of a novel 2-aminotetralin as a mixed dopamine Dl/D2-receptor agonist, whereas part I1 (chapters 4-6) concerns the development of 2-amidotetralins as nonindolic melatonin-receptor agents. 
2 Citations

New, centrally acting dopaminergic agents with an improved oral bioavailability: synthesis and pharmacological evaluation

This chapter describes the synthesis and in vitro pharmacology of a novel series of dopamine receptor ligands, in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine

Impact of substituents on the enantioseparation of racemic 2‐amidotetralins on polysaccharide stationary phases. I. chiralcel OD

The direct enantiomeric separation of 32 racemic 2-amidotetralins on the commercially available tris-(3,5-dimethylphenylcarbamate) derivative of cellulose, coated on silica gel (Chiralcel OD), is



The Development of Potent and Selective D-2 Agonists of the 2-Aminotetralin Group: Their Clinical Applications and their Use in the Isolation of the D-2 Receptor

In addition to the aporphine and ergot analogues the 2-aminotetralin derivatives have been one of the most important groups of compounds which have increased our understanding of the neurobiology of

Synthesis and pharmacology of some 2-aminotetralins. Dopamine receptor agonists.

Data support the idea that the extended conformation for the phenylethylamine moiety of ampmorphine and dopamine is favorable for dopaminergic agonist activity and suggest that an unetherified catechol group may not be essential for such activity.

Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues.

A series of melatonin analogues was synthesized and examined for ovulation-blocking activity, and a pronounced enhancement resulted from halogenation of the 6 position.

Recent advances in central 5-hydroxytryptamine receptor agonists and antagonists.

Improvements in the pharmacology and medicinal chemistry of 5-hydroxytryptamine (5-HT, serotonin) and related agents and the introduction of agents with selective pharmacological actions are shown.

The fate of melatonin in animals.

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.

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.

Cerebral dopamine agonist properties of some 2-aminotetralin derivatives after peripheral and intracerebral administration.

Stereotypical behavioral effects produced by direct intracerebral administration of some of the agents were shown to differ strikingly from responses resulting from peripheral administration, and centrally mediated responses of hyperactivity and sterotypical gnawing-biting head and limb movements were showed to be separable in some test compounds.