Binding of 2,4-substituted morpholines at human D4 dopamine receptors

Article abstract of DOI:10.1016/S0968-0896(97)00176-4

The synthesis of a series of 2,4-disubstituted morpholines is described and their affinities at human dopamine receptors reported. The orally bioavailable 7-azaindole compound 11 has nanomolar affinity at the hD₄ receptor with > 1000-fold selectivity over the hD₂ receptor.