Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine

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...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1989-07, Vol.32 (7), p.1627-1630
Main Authors: Chapleo, C B, Butler, R C, England, D C, Myers, P L, Roach, A G, Smith, C F, Stillings, M R, Tulloch, I F
Format: Article
Language:English
Subjects:
Adrenergic alpha-Agonists
Animals
Brain - drug effects
Clonidine - analogs & derivatives
Clonidine - pharmacology
Heterocyclic Compounds - pharmacology
Male
Rats
Vas Deferens - drug effects
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Summary: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.
ISSN:0022-2623
DOI:10.1021/jm00127a037