Add time:08/30/2019         Source:sciencedirect.com

The ability of a series of adrenergic agents to displace the binding to brain membranes of [3H]WB 4101, a potent α-adrenergic antagonists (WB4101 = 2[2-(2,6-dimethoxyphenoxy)ethylaminomethyl]-1,4-benzodioxane hydrochloride), has been compared with the potency of these agents in stimulating or inhibiting the α-adrenergic component of cyclic AMP accumulation in rat cerebral cortex slices. [3H]WB 4101 rapidly bound to a high affinity site (KD = 2.7nM) in membranes from cerebral cortex Binding came to equilibrium by 2 min at 37°C and was rapidly reversed in the presence of phentolamine. The potencies of adrenergic agents (WB 4101 > phentolamine > naphazoline) in displacing binding of [4H]WB 4101 were comparable to the potencies of these agents as inhibitors of the α-adrenergic component of norepinephrine-stimulated cyclic AMP accumulations. Phenoxybenzamine, clonidine, chlorpromazine and haloperidol were about 10–30 times more potent in inhibiting cyclic AMP accumulation than in displacing [3H]WB 4101 binding. The potency of classical α-adrenergic agonists in displacing WB 4101 (epinephrine > norepinephrine > methoxamine) correlated with the ability of these agonists to increase cyclic AMP levels. Overall a significant correlation (r = 0.87, P < 0.005) was found between WB4101 binding and α-AAadrenergically mediated cyclic AMP accumulation in brain. Several ligands bind to specific sites in brain membranes with α-adrenergic receptor properties. The identificatiom of these binding sites as receptors depends on a correlation of binding with a known α-adrenergic receptor-mediated response in brain. These data demonstrating that WB4101 correlates with norepinephrine-stimulated cyclic AMP accumulation suggest that WB 4101 may bind to the membrane receptor sites mediating the α-adrenergic accumulation of cyclic AMP in rat cerebral cortex.

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