Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands,Chemical Biology & Drug Design

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Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-07-01 , DOI: 10.1111/cbdd.13324
Benhua Zhou _{1,

2} , Kwon Ho Hong ₃ , Min Ji _{4,

5} , Jin Cai _{1,

5}

Affiliation

Two series of hybrid analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined (using the method of radioligand binding assay). Compared to comparator agent BP897, compounds 2a and 2c were found to demonstrate a considerable binding affinity and selectivity for D3 receptor, and especially compound 2h was similarly potent and more selective D3R ligand than BP897, a positive reference. Thus, they may provide valuable information for the discovery and development of highly potent dopamine D3 receptor ligands with outstanding selectivity.

中文翻译：

设计，合成和生物学评估结构受限的杂种类似物，其中包含罗匹尼罗部分作为新型强效和选择性多巴胺D3受体配体

设计，合成和评估了两个系列的杂合类似物，作为多巴胺D3受体的一类新的选择性配体。确定目标化合物的结合亲和力（使用放射性配体结合测定法）。与比较剂BP897相比，发现化合物2a和2c对D3受体表现出相当大的结合亲和力和选择性，尤其是化合物2h与BP897（正参比）具有相似的效力和更高的D3R配体。因此，它们可以为发现和开发具有出色选择性的高效多巴胺D3受体配体提供有价值的信息。

更新日期：2018-07-01

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