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Comparison of central and peripheral alpha1-adrenoceptors

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Summary

A series of alpha-adrenergic agonists and antagonists having diverse chemical structure was examined for both central and peripheral alpha1-adrenoceptor activity. The agonists tested included several novel aminotetralin derivatives which were potent and selective alpha1-agonists. Peripheral alpha1-activity was determined in the isolated rabbit ear artery; central alpha1-receptor affinity was measured as the ability to inhibit 3H-WB 4101 binding to rat brain homogenates. In the agonist series, an excellent correlation between peripheral alpha1-activity and central alpha1-affinity was obtained, providing that partial agonists were excluded. Likewise, the receptor dissociation constant for blockade of the peripheral alpha1-adrenoceptor correlated well with affinity for the central receptor for all of the alphaantagonists. These data support the conclusion that central and peripheral alpha1-adrenoceptors are similar or identical.

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Authors and Affiliations

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

    J. Paul Hieble, Henry M. Sarau, James J. Foley, Robert M. Demarinis & Robert G. Pendleton

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  1. J. Paul Hieble
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  2. Henry M. Sarau
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  3. James J. Foley
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  4. Robert M. Demarinis
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  5. Robert G. Pendleton
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Hieble, J.P., Sarau, H.M., Foley, J.J. et al. Comparison of central and peripheral alpha1-adrenoceptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 318, 267–273 (1982). https://doi.org/10.1007/BF00501164

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  • DOI: https://doi.org/10.1007/BF00501164

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