(R)- and (S)-5-hydroxy-2-(dipropylamino)tetralin (5-OH DPAT): assessment of optical purities and dopaminergic activities.

作者: Anders Karlsson , Curt Pettersson , Lena Björk , Nils-Erik Andén , Uli Hacksell

DOI: 10.1002/CHIR.530020206

关键词: DopaminergicAgonist5-OH-DPATStereoselectivityStereochemistryChemistryTetralinDopamineEnantiomerAntagonist

摘要: Racemic 5-hydroxy-2-(dipropylamino)tetralin (5-OH DPAT), a potent and selective dopamine (DA) D2-receptor agonist, was resolved into the enantiomers by new method. The of 5-OH DPAT were determined chiral ion-pair chromatography using N-benzyloxycarbonylglycyl-L-proline as counter ion. enantiomeric purity (R)-5-OH found to be greater than 99.7%. ability change rat brain DOPA levels evaluated in vivo. results indicate that is weakly DA antagonist.

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