Leopoldo Marcello, Lacivita Enza, Passafiume Elena, Contino Marialessandra, Colabufo Nicola A, Berardi Francesco, Perrone Roberto
Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Via Orabona, 4, 70125 Bari, Italy.
J Med Chem. 2007 Oct 4;50(20):5043-7. doi: 10.1021/jm070721+. Epub 2007 Sep 12.
Sixteen long-chain arylpiperazines bearing the fluorescent moiety 2-phenylimidazo[1,2-a]pyridine were synthesized as fluorescent dopamine D3 receptors ligands (385 nM < Ki < 0.72 nM). The most potent D3 compounds 15a and 19a (Ki = 1.6 and 0.72 nM, respectively) showed good Stokes shift and high quantum yield in ethanol (Phi = 0.74 and 0.66, respectively). In the first attempt, 15a was unable to visualize D3 receptors expressed in CHO cells by epifluorescence microscopy.
合成了16种带有荧光部分2-苯基咪唑并[1,2-a]吡啶的长链芳基哌嗪作为荧光多巴胺D3受体配体（385 nM < Ki < 0.72 nM）。最有效的D3化合物15a和19a（Ki分别为1.6和0.72 nM）在乙醇中表现出良好的斯托克斯位移和高量子产率（分别为Phi = 0.74和0.66）。在首次尝试中，15a无法通过落射荧光显微镜观察到CHO细胞中表达的D3受体。
