Erowid References Database
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Weinreich P, Seeman P.
“Binding Of Adrenergic Ligands ([3h]clonidine And [3H]WB-4101) To Multiple Sites In Human Brain”.
Biochemical Pharmacology. 1981;30(22):311-312.
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Abstract
In order to identify alpha-adrenoceptors in post-mortem human brain and to detect the possible existence of multiple types of binding sites for adrenergic [3H]ligands, we studied the binding of [3H]clonidine and [3H]WB-4101 to human brain cerebral cortex, hippocampus, hypothalamus and striatum. Frontal cortex revealed two binding sites for [3H]clonidine (with KD values of approximately 1 and 8nM), as indicated by the biphasic Scatchard plot, the biphasic pattern of dissociation kinetics and the biphasic inhibition by phentolamine on the binding of [3H]clonidine, the high-affinity site was heat-labile. Two high-affinity binding sites for [3H]WB-4101 were also detected in the human frontal cortex (with KD values of about 0.09 and B5 nM), as revealed by a biphasic pattern of dissociation. A third site with low affinity binding for [3H]WB-4101 was detected by the biphasic inhibition by phentolamine (as well as by WB-4101 and prazosin) on the binding of [3H]WB-4101. The three other brain regions revealed very similar patterns exhibited by the frontal cortex, except that the density of the [3H]clonidine sites (of either high or low affinity) was highest in the hypothalamus, whereas the density of [3H]W13-4101 sites was highest in the hippocampus.
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