A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Synthesis and pharmacological properties of 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)imidazole, a silicon analogue of atipamezole
Tekijät: Heinonen P, Sipila H, Neuvonen K, Lonnberg H, Cockcroft VB, Wurster S, Virtanen R, Savola MKT, Salonen JS, Savola JM
Kustantaja: EDITIONS SCIENTIFIQUES ELSEVIER
Julkaisuvuosi: 1996
Lehti:: European Journal of Medicinal Chemistry
Tietokannassa oleva lehden nimi: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Lehden akronyymi: EUR J MED CHEM
Vuosikerta: 31
Numero: 9
Aloitussivu: 725
Lopetussivu: 729
Sivujen määrä: 5
ISSN: 0223-5234
DOI: https://doi.org/10.1016/0223-5234(96)85882-X
Tiivistelmä
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 alpha(2)-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.
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 alpha(2)-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.