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Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine. 1989
C B Chapleo, and
R C Butler, and
D C England, and
P L Myers, and
A G Roach, and
C F Smith, and
M R Stillings, and
I F Tulloch
Department of Pharmacology, Reckitt & Colman plc, Pharmaceutical Division, Kingston-upon-Hull, U.K.
A 1,4-dioxane analogue (1) of the alpha 2-adrenoreceptor partial agonist clonidine (2) has previously been shown to possess an interesting but complex pharmacological profile. In this study, from a series of other heterocyclic analogues of clonidine, the 1,4-oxazines 6 and 12 were found to resemble 1 in that they are partial alpha 2-agonists in the periphery and are excluded from the central nervous system. However, when given directly into the brain, they behave as pure alpha 2-antagonists.
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