支链 3-(1H-咪唑-4-基)丙基 N- 烷基氨基甲酸酯的组胺 H3 和 H4 受体亲和力。
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
机构信息
Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, 30-688 Kraków, Poland.
出版信息
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5. doi: 10.1016/j.bmcl.2009.10.005. Epub 2009 Oct 6.
PMID:19846299
Abstract
A series of imidazole-containing (non-)chiral carbamates were tested at human histamine H(3) receptor (H(3)R). All compounds displayed K(i) values below 100 nM. A trend for a stereoselectivity at human H(3)R was observed for the chiral alpha-branched ligands. Selected compounds were also tested at human histamine H(4) receptor and showed moderate to weak affinities (118-1460 nM).
摘要
一系列含咪唑的（非）手性氨基甲酸酯在人源组胺 H（3）受体（H（3）R）上进行了测试。所有化合物的 K(i) 值均低于 100 nM。对于手性的α-支链配体，在人源 H（3）R 上观察到了立体选择性的趋势。选择的化合物也在人源组胺 H（4）受体上进行了测试，显示出中等至弱的亲和力（118-1460 nM）。
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