当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > 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.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Schlotter K,Boeckler F,Hübner H,Gmeiner P

doi

10.1021/jm050170s

keywords:

subject

Has Abstract

pub_date

2005-06-02 00:00:00

pages

3696-9

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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