Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
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奇特的生物等排体：茂金属衍生的 G 蛋白偶联受体配体，具有亚纳摩尔的结合亲和力和新颖的选择性特征。
DOI：
10.1021/jm050170s
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发表时间：
2005
影响因子：
7.3
通讯作者：
P. Gmeiner
中科院分区：
文献类型：
--
作者：
Karin Schlotter;F. Boeckler;H. Hübner;P. Gmeiner
茂金属衍生的生物等排体导致 G 蛋白偶联受体配体结合力异常强，表明受体排除体积具有显着的可塑性。二茂铁甲酰胺的新颖结合特征结合了多巴胺 D4 受体的亚纳摩尔 Ki 值（1a，0.52 nM；1b，0.63 nM）与超强血清素 5-羟色胺1A（1a，0.50 nM）和多巴胺 D3 受体结合（1b，0.64 nM）以及选择性 D4 激动剂特性 钌茂 1c 可能是高度有益的中枢神经系统活性药物的起点。
Metallocene-derived bioisosteres lead to exceptionally strong binding G-protein-coupled receptor ligands, indicating substantial plasticity of the receptor excluded volume. Novel binding profiles of ferrocenylcarboxamides combining subnanomolar Ki values for the dopamine D4 receptor (1a, 0.52 nM; 1b, 0.63 nM) with superpotent serotonin 5-hydroxytryptamine1A (1a, 0.50 nM) and dopamine D3 receptor binding (1b, 0.64 nM) and selective D4 agonist properties of the ruthenocene 1c may be a starting point for highly beneficial central nervous system active drugs.