| 摘要 |
Described herein are D4 receptor-selective compounds of the general formula: <IMAGE> wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is selected from CH2, O, NH, S, C=O, CH-OH, CH-N(C1-4alkyl)2, C=CHCl, C=CHCN, N-C1-4alkyl, N-acetyl, SO2and SO; X2 - - - is selected from N=, CH2-, CH=, C(O)-, O-, and S-; n is 1 or 2; R1 is selected from H and an amino acid side chain; R2 is selected from H, OH, C1-9alkyl, C1-9alkoxy, and benzyloxy; and R3 is selected from H, OH, halo, cyano, C1-4alkyl, C1-4alkoxy, phenoxy, benzyloxy, =O, =S, C1-4alkylsulfonyl, C1-4alkylsulfonyl, C1-4alkylthio, amino, and aminocarbonyl; 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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