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 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.
Chapleo
C B
CB
Department of Pharmacology, Reckitt & Colman plc, Pharmaceutical Division, Kingston-upon-Hull, U.K.
Butler
R C
RC
England
D C
DC
Myers
P L
PL
Roach
A G
AG
Smith
C F
CF
Stillings
M R
MR
Tulloch
I F
IF
D000316:Adrenergic alpha-Agonists; D000818:Animals; D001921:Brain / Q000187:drug effects; D003000:Clonidine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000494:pharmacology*; D008297:Male; D051381:Rats; D014649:Vas Deferens / Q000187:drug effects
D000316:Adrenergic alpha-Agonists; D006571:Heterocyclic Compounds; C039190:2-(6-(1,4-benzodioxanyl)amino)imidazoline maleate; D003000:Clonidine