3-AMINOMETHYLBIPHENYLS - A NEW CLASS OF DOPAMINE-RECEPTOR LIGANDS

A series of 3-aminomethylbiphenyls were prepared in three steps from 3 -phenylbenzoic acid and their affinities for the D-2, D-3 and D-4 dopa mine receptor subtypes determined. Most of the compounds described con tained unique amine subunits of known dopaminergic agents. The compoun ds containing the amino tails present in the antipsychotic drugs halop eridol, pimozide and miliperidine displayed selectivity for the D-2 re ceptor. Five-fold selectivity for the D-4 receptor was observed in the compound 1-(3-biphenyl)-4-(2-pyrimidyl)piperazine. This selectivity f or D-4 vs. D-2 receptors is comparable to that observed with the atypi cal antipsychotic clozapine.