Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines

Attila Sipos, C. Csutorás, Sándor Berényi, Ain Uustare, Ago Rinken

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

We have synthesized novel 2-O-substituted apomorphines with both different lengths of lipophilic alkyl chains and alkyl chains carrying free hydroxyl groups. Two bis-apomorphines formed as side products of the reactions with diols were isolated and characterized as well. The neuropharmacological profile of all these new compounds were investigated with respect to their binding affinities and activities to dopamine D2 and D1 receptors. The obtained data pointed to the fact that, in the examination of dopaminergic activities of 2-substituted apomorphines, the lipophilicity of the substituent is more important than its spatial parameters.

Original languageEnglish
Pages (from-to)4563-4568
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number8
DOIs
Publication statusPublished - Apr 15 2008

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Dopamine D1 Receptors
Dopamine D2 Receptors
Hydroxyl Radical

Keywords

  • 2-Alkoxyapomorphines
  • Alkyl-type hydroxyl
  • Apomorphine
  • Bis-apomorphines
  • D/D receptor selectivity
  • Dopamine receptor binding activity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines. / Sipos, Attila; Csutorás, C.; Berényi, Sándor; Uustare, Ain; Rinken, Ago.

In: Bioorganic and Medicinal Chemistry, Vol. 16, No. 8, 15.04.2008, p. 4563-4568.

Research output: Contribution to journalArticle

Sipos, Attila ; Csutorás, C. ; Berényi, Sándor ; Uustare, Ain ; Rinken, Ago. / Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines. In: Bioorganic and Medicinal Chemistry. 2008 ; Vol. 16, No. 8. pp. 4563-4568.
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