Journal of Medicinal Chemistry p. 666 - 670 (1982)
Update date:2022-07-30
Topics:
Caroon, Joan M.
Clark, Robin D.
Kluge, Arthur F.
Olah, Ronald
Repke, David B.
et al.
Several 2-<(1,4-benzodioxan-2-yl)alkyl>imidazoles were prepared and evaluated for their blocking activity and relative selectivity on presynaptic (α2) and postsynaptic (α1) receptors in the isolated rat vas deferens. 1-Ethyl-2-<(1,4-benzodioxan-2-yl)methyl>imidazole (13) was the most selective α2-adrenoceptor antagonist of the series and was for practical purposes, devoid of α1-adrenoceptor antagonist activity.The lipophilicity of 13 (log D = 2.31) indicated that it would have an excellent chance to enter the central nervous system.Compound 13 was selected for clinical evaluation as an antidepressant agent.
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Doi:10.1002/hlca.19810640816
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