| Abstract: | 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 similarly 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. |
