title: alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
abstract: Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subtype selective agonists have been identified.
authors.affiliation: GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.mjb45288@glaxowellcome.com
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bishop
authors.forename: Kevin A
authors.initials: KA
authors.lastname: Barvian
authors.forename: Judd
authors.initials: J
authors.lastname: Berman
authors.forename: Eric C
authors.initials: EC
authors.lastname: Bigham
authors.forename: Deanna T
authors.initials: DT
authors.lastname: Garrison
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Gobel
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Hodson
authors.forename: Paul E
authors.initials: PE
authors.lastname: Irving
authors.forename: James A
authors.initials: JA
authors.lastname: Liacos
authors.forename: Frank
authors.initials: F
authors.lastname: Navas
authors.forename: David L
authors.initials: DL
authors.lastname: Saussy
authors.forename: Jason D
authors.initials: JD
authors.lastname: Speake
mesh_terms: D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D006801:Humans; D006860:Hydrogen Bonding; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D010647:Phenyl Ethers / Q000138:chemical synthesis* / Q000494:pharmacology*; D018340:Receptors, Adrenergic, alpha-1; D011994:Recombinant Proteins; D013329:Structure-Activity Relationship; D014550:Urinary Incontinence, Stress / Q000517:prevention & control
chemical_list: C547713:ADRA1A protein, human; D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D010647:Phenyl Ethers; D018340:Receptors, Adrenergic, alpha-1; D011994:Recombinant Proteins