2-(4,5-Dihydroimidazol-2-yl)benzimidazoles as highly selective imidazoline I2/adrenergic alpha2 receptor ligands |
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| Authors: | Saczewski Francieszek Tabin Piotr Tyacke Robin J Maconie Alys Saczewski Jarosław Kornicka Anita Nutt David J Hudson Alan L |
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| Affiliation: | Department of Chemical Technology of Drugs, Medical University of Gdańsk, 80-416 Gdańsk, Poland. saczew@amg.gda.pl |
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| Abstract: | 2-(4,5-Dihydroimidazol-2-yl)benzimidazoles have been identified as selective imidazoline I2/alpha2-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/alpha2 selectivity ratio=4226 and 5649, respectively. An evidence has been obtained that pKa value influences considerably the I2/alpha2-selectivity ratio of this class of imidazoline I2 receptor ligands. |
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