title: Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
abstract: 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.
authors.affiliation: Department of Pharmacology, Reckitt & Colman plc, Pharmaceutical Division, Kingston-upon-Hull, U.K.
authors.forename: C B
authors.initials: CB
authors.lastname: Chapleo
authors.forename: R C
authors.initials: RC
authors.lastname: Butler
authors.forename: D C
authors.initials: DC
authors.lastname: England
authors.forename: P L
authors.initials: PL
authors.lastname: Myers
authors.forename: A G
authors.initials: AG
authors.lastname: Roach
authors.forename: C F
authors.initials: CF
authors.lastname: Smith
authors.forename: M R
authors.initials: MR
authors.lastname: Stillings
authors.forename: I F
authors.initials: IF
authors.lastname: Tulloch
mesh_terms: 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
chemical_list: D000316:Adrenergic alpha-Agonists; D006571:Heterocyclic Compounds; C039190:2-(6-(1,4-benzodioxanyl)amino)imidazoline maleate; D003000:Clonidine