ISSN:
1432-1912
Keywords:
Alpha1-adrenoceptors
;
2-Aminotetralins
;
Rabbit ear artery
;
3H-WB 4101 binding
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00501164
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