Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors

Article abstract of DOI:10.1016/S0960-894X(98)00138-3

We synthesized 20 and 21 as conformationally constrained analogues of the dopamine receptor antagonist SKF-83742, as well as analogues 6-9, 16, and 18-22. Although 20 and 21 were inactive, 7, 9, and 19 showed strong binding to D-1, D-2, S-2, and α-1 receptors, as well as antipsychotic activity in vivo.