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Effects of ring substitution on the pre- and postjunctional alpha-adrenergic activity of aryliminoimidazolidines

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Summary

The pre- and postjunctional α-adrenergic agonist potency of a series of aryliminoimidazolidines was determined in the isolated rabbit ear artery. This series included clonidine, an antihypertensive agent thought to act by stimulating brainstem α-receptors and known to be a preferentially prejunctional α-adrenergic agonist. Although all of the compounds acted preferentially on the prejunctional α-adrenoceptor, ring substitution had a dramatic effect on both potency and the degree of selectivity. 2-(3,4-Dihydroxyphenylimino) imidazolidine was both the most potent and most selective prejunctional α-agonist in this series.

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Authors and Affiliations

  1. Research and Development Division, Smith Kline and French Laboratories, 19101, Philadelphia, Pennsylvania, USA

    J. Paul Hieble & Robert G. Pendleton

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  1. J. Paul Hieble
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  2. Robert G. Pendleton
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Hieble, J.P., Pendleton, R.G. Effects of ring substitution on the pre- and postjunctional alpha-adrenergic activity of aryliminoimidazolidines. Naunyn-Schmiedeberg's Arch. Pharmacol. 309, 217–224 (1979). https://doi.org/10.1007/BF00504753

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  • DOI: https://doi.org/10.1007/BF00504753

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