Phenoxybenzamine is more potent in inactivating alpha 1- than alpha 2-adrenergic receptor binding sites.

Abstract

The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. Treatment with phenoxybenzamine caused an irreversible, dose-dependent decrease in the density of both alpha 1- and alpha 2-adrenergic receptors. Phenoxybenzamine was approximately 250-fold more potent at decreasing alpha 1-adrenergic receptor density than it was at decreasing alpha 2-adrenergic receptor density.

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@article{Minneman1983PhenoxybenzamineIM, title={Phenoxybenzamine is more potent in inactivating alpha 1- than alpha 2-adrenergic receptor binding sites.}, author={Kenneth P. Minneman}, journal={European journal of pharmacology}, year={1983}, volume={94 1-2}, pages={171-4} }