alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
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.
Bishop
Michael J
MJ
GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.mjb45288@glaxowellcome.com
Barvian
Kevin A
KA
Berman
Judd
J
Bigham
Eric C
EC
Garrison
Deanna T
DT
Gobel
Michael J
MJ
Hodson
Stephen J
SJ
Irving
Paul E
PE
Liacos
James A
JA
Navas
Frank
F
Saussy
David L
DL
Speake
Jason D
JD
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
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