2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
2-(Anilinomethyl)imidazolines with 2'-esters or 2'-amides are potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The size and shape of the ortho substituent can have significant effects on the potency, efficacy, and subtype selectivity of these 2-(anilinomethyl)imidazolines. alpha(1A)-subtype selective agonists have been identified.
Bishop
M J
MJ
GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. mjb45288@glaxowellcome.com
Berman
J
J
Bigham
E C
EC
Garrison
D T
DT
Gobel
M J
MJ
Hodson
S J
SJ
Irving
P E
PE
Liacos
J A
JA
Minick
D J
DJ
Navas
F
F
Saussy
D L
DL
Speake
J D
JD
D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000737:chemistry / Q000494:pharmacology*; D000577:Amides / Q000737:chemistry; D002264:Carboxylic Acids / Q000737:chemistry*; D004952:Esters / Q000737:chemistry; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D000577:Amides; D002264:Carboxylic Acids; D004952:Esters; D007093:Imidazoles