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In vitro studies on 6-fluoronoradrenaline at several peripheral sympathetic neuroeffector junctions

  • N. B. Shepperson
  • T. Purcell
  • R. Massingham
  • S. Z. Langer
Article

Summary

A comparison of the effects of noradrenaline and 6-fluoronoradrenaline has been made at several peripheral sympathetic neuroeffector junctions. In the rat vas deferens preparation in the presence of 1 μM cocaine, 6-fluoronor-adrenaline was found to be about 9 times more potent than noradrenaline as an agonist at presynaptic inhibitory α2-adrenoceptors. In the rabbit aorta, 6-fluoronoradrenaline had approximately one tenth of the potency of noradrenaline in stimulating the postsynaptic α1-adrenoceptors. Furthermore 6-fluoronoradrenaline, in contrast to previous reports, appears to be a substrate for the neuronal uptake process since exposure to cocaine potentiated the inhibition of the twitch response of the vas deferens by 6-fluoronoradrenaline. In addition, 6-fluoronoradrenaline increased the spontaneous outflow of radioactivity from rabbit pulmonary artery strips prelabelled with 3H-noradrenaline and this increase was blocked by cocaine (30μM).

These results demonstrate that 6-fluoronoradrenaline is a preferential α2-adrenoceptor agonist which is a substrate for the neuronal uptake process in peripheral sympathetically innervated smooth muscle preparations.

Key words

6-Fluoronoradrenaline Sympathetic neurotransmission Neuronal uptake α1- and α2-Adrenoceptors 

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Copyright information

© Springer-Verlag 1981

Authors and Affiliations

  • N. B. Shepperson
    • 1
  • T. Purcell
    • 2
  • R. Massingham
    • 1
  • S. Z. Langer
    • 1
  1. 1.Department of BiologyLaboratoires d'Etudes et de Recherches SynthélaboParisFrance
  2. 2.Department of ChemistryLaboratoires d'Etudes et de Recherches SynthélaboParisFrance

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