2-(4, 5-Dihydroimidazol-2-yl) benzimidazoles as highly selective imidazoline I 2/adrenergic α 2 receptor ligands

…, P Tabin, RJ Tyacke, A Maconie, J Sączewski…

文献索引：Saczewski, Francieszek; Tabin, Piotr; Tyacke, Robin J.; Maconie, Alys; Saczewski, Jaroslaw; Kornicka, Anita; Nutt, David J.; Hudson, Alan L. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 19 p. 6679 - 6685

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被引用次数: 9

摘要

2-(4, 5-Dihydroimidazol-2-yl) benzimidazoles have been identified as selective imidazoline I2/α2-adrenoceptor ligands. 4-Methyl (2) and 4-chloro (4) derivatives display I2 affinity at nanomolar concentration (Ki= 4.4 and 17.7 nM, respectively) and high I2/α2 selectivity ratio= 4226 and 5649, respectively. An evidence has been obtained that pKa value influences considerably the I2/α2-selectivity ratio of this class of imidazoline I2 receptor ligands.