Abstract
Alpha adrenergic receptor sites in mammalian brain tissue can be labeled by the binding of [3H]WB-4101 (2-([2′,6′-dimethoxy] phenoxyethylamino) methyl benzodioxan), a potent α-adrenergic antagonist. Numerous neuroleptic drugs of phenothiazine, butyrophenone and thioxanthene classes are potent in competing for [3H]WB-4101 binding, with affinities resembling those of classic α-antagonists such as phentolamine and phenoxybenzamine. The potencies of neuroleptics in competing for WB-4101 binding sites correlate closely with their potencies in antagonizing norepinephrine and epinephrine induced lethality in rats, confirming that affinity for WB-4101 binding sites predicts α-receptor antagonism in vivo. The relative affinities of neuroleptics for WB-4101 binding sites and for dopamine receptors as labeled by [3H]haloperidol provides an index of the relative propensities of these drugs for eliciting autonomic side effects such as orthostatic hypotension and sedation.
Original language | English (US) |
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Pages (from-to) | 549-556 |
Number of pages | 8 |
Journal | Neuropharmacology |
Volume | 16 |
Issue number | 9 |
DOIs | |
State | Published - Sep 1977 |
Keywords
- Alpha receptor
- binding
- hypotension
- neuroleptics
- sedation
ASJC Scopus subject areas
- Pharmacology
- Cellular and Molecular Neuroscience