title: Alpha-adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists.
abstract: The synthesis and pharmacological activity of a series of 2-substituted derivatives of the selective alpha 2-adrenoreceptor antagonist idazoxan (RX 781094) is described. Substitution in this position by alkyl, alkenyl, cycloalkenyl, and alkoxy groups in many cases gives compounds whose potencies and selectivities are significantly greater than those of the parent compound.
authors.forename: M R
authors.initials: MR
authors.lastname: Stillings
authors.forename: C B
authors.initials: CB
authors.lastname: Chapleo
authors.forename: R C
authors.initials: RC
authors.lastname: Butler
authors.forename: J A
authors.initials: JA
authors.lastname: Davis
authors.forename: C D
authors.initials: CD
authors.lastname: England
authors.forename: M
authors.initials: M
authors.lastname: Myers
authors.forename: P L
authors.initials: PL
authors.lastname: Myers
authors.forename: N
authors.initials: N
authors.lastname: Tweddle
authors.forename: A P
authors.initials: AP
authors.lastname: Welbourn
authors.forename: J C
authors.initials: JC
authors.lastname: Doxey
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D004146:Dioxanes / Q000138:chemical synthesis / Q000494:pharmacology*; D004147:Dioxins / Q000494:pharmacology*; D019329:Idazoxan; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D013329:Structure-Activity Relationship; D013569:Synapses / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
chemical_list: D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D004147:Dioxins; D011942:Receptors, Adrenergic, alpha; D019329:Idazoxan