European Journal of Clinical Pharmacology

, Volume 44, Issue 1, pp 93–95 | Cite as

Oxaprotiline: enantioselective noradrenaline uptake inhibition indicated by intravenous amine pressor tests but not α2-adrenoceptor binding to intact platelets in man

  • I. W. Reimann
  • L. Firkusny
  • K. H. Antonin
  • P. R. Bieck
Short Communications

Summary

The optically active isomers of the racemic tetracyclic antidepressant oxaprotiline, R (−) oxaprotiline CGP 12 103 A (levoprotiline) and the S (+) oxaprotiline CGP 12 104 A, have been used as tools for a methodological Phase I study.

Only the S (+) enantiomer CGP 12 104 A inhibits noradrenaline uptake.

Intravenous amine pressor tests and ex vivo measurement of α2-adrenoceptor binding to intact human platelets were compared with respect to their reliability in indicating CGP 12 104 A-induced amine uptake inhibition and possibly associated α2-receptor down-regulation in healthy subjects.

α2-Adrenoceptor binding on intact human platelets did not distinguish between CGP 12 104 A and CGP 12 103 A.

However, amine pressor tests reflected the amine uptake inhibiting effect of CGP 12 104 A as a 5-fold decrease in tyramine pressor sensivity and a 5-fold increase in noradrenaline pressor sensitivity.

Key words

Oxaprotiline Levoprotiline noradrenaline uptake inhibitors enantiomers CGP 12 103 A CGP 12 104 A amine pressor tests α2-adrenoceptor binding intact human platelets 

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Copyright information

© Springer-Verlag 1993

Authors and Affiliations

  • I. W. Reimann
    • 1
  • L. Firkusny
    • 1
  • K. H. Antonin
    • 1
  • P. R. Bieck
    • 1
  1. 1.Human Pharmacology Institute Ciba-GeigyTübingenFRG

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