Effect of 1,4-dioxanyl substitution on the adrenergic activity of some standard α-adrenoreceptor agents

Article abstract of DOI:10.1016/0223-5234(89)90031-7

A preliminary communication reported on the pharmacology of the potent partial α₂-agonist (2-(1,4-benzodioxan-6-ylamino)-2-imidazoline, a 1,4-dioxan derivative of clonidine.Its degree of agonism/antagonism depended upon the peripheral or central α₂-adrenoreceptor system studied.It was of interest to discover whether a similar substitution of the 1,4-dioxan moiety in other standard α-adrenergic agents would similary produce high affinity compounds of complex pharmacological profile.The same substitution when introduced into guanfacine, fenmetazole and tolazoline resulted in unpredictable changes in profile with a reduction in α-affinity. - α₂-adrenoreceptors/antagonism/agonism/clonidine derivatives/1,4-dioxan derivatives