| 摘要 |
Described herein are D4 receptor-selective compounds of the general formula: <IMAGE> wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is selected from O, S, SO, SO2, CH2, C=O, CH-OH, CH-N(C1-4alkyl)2, C=CHCl, and C=CHCN; X2--- is selected from N=, CH2-, CH= and C(O)-; n is 1 or 2; R1 is selected from H and the alpha -carbon side chain of an amino acid; R2 and R3 are selected independently from H, OH, -NH2, -C(O)NH2=O, =S,halo,cyano, C1-9alkyl, C1-9alkoxy, C1-4alkylS-, C1-4alkylSO-, C1-4alkylSO2-, phenoxy, benzyloxy and piperonyloxy; and H* is in either the R- or the S-configuration, and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
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