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.
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References
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© 1991 Springer-Verlag
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Langer, S.Z., Angel, I. (1991). Pre- and postsynaptic alpha-2 adrenoceptors as target for drug discovery. In: Bönisch, H., Graefe, KH., Langer, S.Z., Schömig, E. (eds) Recent Advances in Neuropharmacology. Journal of Neural Transmission, vol 34. Springer, Vienna. https://doi.org/10.1007/978-3-7091-9175-0_22
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DOI: https://doi.org/10.1007/978-3-7091-9175-0_22
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