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Selective labeling of alpha-noradrenergic receptors in rat brain with [3H]dihydroergokryptine.
Authors:D A Greenberg  S H Snyder
Institution:Departments of Pharmacology and Experimental Therapeutics and Psychiatry and Behavioral Sciences Johns Hopkins University School of Medicine Baltimore, Maryland 21205, USA
Abstract:Using concentrations of 3H] dihydroergokryptine between 0.1 and 5 nM, saturable binding can be demonstrated in rat cerebral cortical membranes with a dissociation constant (KD) of about 0.8 nM. α-Noradrenergic agonists and antagonists compete for the sites labeled by these low concentrations of 3H] dihydroergokryptine with relative potencies characteristics of classical α-noradrenergic receptors. The very low potency of serotonin in competing for these binding sites indicates that, in contrast to findings with higher concentrations of 3H] DHE, low concentrations do not label serotonin receptors. Moreover, the low potency of dopamine in competing for 3H] dihydroergokryptine binding in both striatal and cortical membranes indicates that no detectable portion of binding is associated with postsynaptic dopamine receptors.
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