α-Adrenoreceptor Reagents. 3. Synthesis of Some 2-Substituted 1,4-Benzodioxans as Selective Presynaptic α2-Adrenoreceptor Antagonists

Article abstract of DOI:10.1021/jm00146a013

The synthesis and pharmacological activity of a series of 2-substituted derivatives of the selective α₂-adrenoreceptor antagonist idazoxan (RX 781094) is described.Substitution in this position by alkyl, alkenyl, cycloalkenyl, and alkoxy groups in many cases gives compounds whose potencies and selectivities are significantly greater than those of the parent compound.