Oct 14, 1983

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

European Journal of Pharmacology
K P Minneman

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.

Mentioned in this Paper

Yohimbin Spiegel
Phenoxybenzamine Hydrochloride
August Rats
Rauwolscine
Adrenergic Receptor
BE 2254, (+-)-isomer
Tetralones
Insula of Reil
Cerebral Cortex
Phenoxybenzamine

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.