Synthesis and pharmacological properties of 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)imidazole, a silicon analogue of atipamezole

Article abstract of DOI:10.1016/0223-5234(96)85882-X

4(5)-(2-Ethyl-2,3-dihydro-2-silainden-2-yl)imidazole 2a, 4(5)-(2-methyl-2,3-dihydro-2-silainden-2-yl)imidazole 2b and 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)-2-methylimidazole 2c, C2 silicon analogues of the commercially available α₂-adrenergic receptor antagonist atipamezole 1, were prepared and their pharmacological properties were evaluated. The results show that 2a retained significant affinity for the receptors, and the in vivo pharmacokinetic properties of 2a were comparable to those of 1.