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Pre- and postsynaptic alpha-2 adrenoceptors as target for drug discovery

  • S. Z. Langer
  • I. Angel
Conference paper
Part of the Journal of Neural Transmission book series (NEURAL SUPPL, volume 34)

Summary

The presynaptic terminal autoreceptors which modulate the release of noradrenaline through a negative feed-back mechanism correspond to the α2-subtype of adrenoceptors. These receptors are also present post- synaptically in the pancreatic islets were they mediate inhibition of the glucose- induced release of insulin. The sympathetic innervation of the pancreatic islets involves α2-adrenoceptors both presynaptically as well as postsynaptically. SL 84.0418 is a novel α2-adrenoceptor antagonist with preferential effects in the periphery and with at least a 10-fold higher selectivity ratio between α2 and ar adrenoceptors when compared with idazoxan. SL 84.0418 antagonizes the hyperglycemia and the inhibition of insulin release induced by the α2- adrenoceptor agonist UK 14304. The administration of SL 84.0418 significantly reduces the glucose evoked hyperglycemia in several species including man. It is proposed that SL 84.0418 may represent a useful and novel hypoglycemic drug in the treatment of type II diabetes.

Keywords

Insulin Release Selectivity Ratio Rabbit Pulmonary Artery Canine Saphenous Vein High Selectivity Ratio 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer-Verlag 1991

Authors and Affiliations

  • S. Z. Langer
    • 1
  • I. Angel
    • 1
  1. 1.Department of BiologySynthélabo Recherche (LERS)Paris Cédex 13France

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