Synthesis of Some Phenothiazine Derivatives as Potential Affinity Ligands for the Central Dopamine Receptors

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Abstract
Syntheses of several phenothiazine ligands as potential affinity probes for the D1- and D2-dopamine receptors derived from 4-(3-(10-(2-trifluorornethyl) phenothiazinyl) propyl)-1-(2-aminoethyl)-piperazine hydrochloride are described and their interactions with D1 and D2-dopamine receptors of the bovine caudate nucleus have been characterized. The bromoacetylamido-, maleinimido-, and isothiocyanato-derivatives expressed low selectivity and moderate affinity for both categories of dopamine receptors. 4-(3-(10-(2-Trifluoromethyl) phenothiazinyl)propyl)-1-(2-(isothiocyanatobenzoyl)ethyl)-piperazine hydrochloride did not discriminate among the two subclasses of the dopamine receptors, but showed an extremely strong irreversible binding to the D1-receptors and thus is promising as a highly specific affinity ligand for biochemical and pharmacological studies of the D1-dopamine receptors.