A series of 1-phenylbenzazepines containing bromine or chlorine substituents at the ortho position of the appended phenyl ring (2′-monosubstituted or 2′,6′- disubstituted patterns) were synthesized and evaluated for affinity towards dopamine D₁R, D₂R and D₅R. As is typical of the 1-phenylbenzazepine scaffold, the compounds displayed selectivity towards D₁R and D₅R; analogs generally lacked affinity for D₂R. Interestingly, 2′,6′-dichloro substituted analogs showed modest D₅R versus D₁R selectivity whereas this selectivity was reversed in compounds with a 2′-halo substitution pattern. Compound 10a was identified as a D₁R antagonist (K_i = 14 nM; IC₅₀ = 9.4 nM).

合成了一系列在附加苯环的邻位（2'-单取代或 2',6'-双取代模式）含有溴或氯取代基的 1-苯基苯并氮杂并评估了对多巴胺 D ₁ R、D ₂ R 的亲和力和 D ₅ R。作为典型的 1-苯基苯并氮杂支架，这些化合物对 D ₁ R 和 D ₅ R表现出选择性；类似物通常对 D ₂ R缺乏亲和力。有趣的是，2',6'-二氯取代的类似物显示出适度的 D ₅ R 与 D ₁ R 选择性，而这种选择性在具有 2'-卤素取代模式的化合物中相反。化合物10a被鉴定为D ₁ R拮抗剂（K _i  = 14 nM；IC ₅₀  = 9.4 nM）。