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A series of alpha-adrenergic agonists and antagonists having diverse chemical structure was examined for both central and peripheral alpha 1-adrenoceptor activity. The agonists tested included several novel aminotetralin derivatives which were potent and selective alpha 1-agonists. Peripheral alpha 1-activity was determined in the isolated rabbit ear artery; central alpha 1-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 alpha 1-activity and central alpha 1-affinity was obtained, providing that partial agonists were excluded. Likewise, the receptor dissociation constant for blockade of the peripheral alpha 1-adrenoceptor correlated well with affinity for the central receptor for all of the alpha-antagonists. These data support the conclusion that central and peripheral alpha 1-adrenoceptors are similar or identical.
J P Hieble, and
H M Sarau, and
J J Foley, and
R M Demarinis, and
R G Pendleton
January 1982,
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J P Hieble, and
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J J Foley, and
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R G Pendleton
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J P Hieble, and
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J P Hieble, and
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J P Hieble, and
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J P Hieble, and
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J P Hieble, and
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J P Hieble, and
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R G Pendleton
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