期刊
CHEMBIOCHEM
卷 5, 期 4, 页码 508-518出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.200300784
关键词
antagonists; dopamines; radiopharmaceuticals; schizophrenia; tetrahydroisoquinoline
Based on N-alkylated 1,2,3,4-tetrahydroisoquinoline derivatives, which are structurally related: to the partial agonist BP 897, a series of novel, selective dopamine D-3 receptor antagonists has been synthesised. Derivatisation included changes in the arylamide moiety and the tetrahydroisoquinoline substructure leading to compounds with markedly improved selectivities and affinities in the low nanomolar concentration range. From the 55 structures presented here, (E)-3-(4-iodophenyl)-N-(4-(1,2,3,4-tetrahydroisoquinolin-2-yl)butyl)actylamide (51) has high affinity (K-i(hD(3))=12 nM) and a 123-fold preference for the D-3 receptor relative to the D-2 receptor subtype. Its pharmacological profile offers the prospect of a novel radioligand as a tool for various dopamine D-3-receptor-related in vitro and in vivo investigations.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据