3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
The 3-pyridylethanolamine L-757,793 is a potent beta 3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta 1 and beta 2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
Naylor
E M
EM
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Colandrea
V J
VJ
Candelore
M R
MR
Cascieri
M A
MA
Colwell
L F
LF
Deng
L
L
Feeney
W P
WP
Forrest
M J
MJ
Hom
G J
GJ
MacIntyre
D E
DE
Strader
C D
CD
Tota
L
L
Wang
P R
PR
Wyvratt
M J
MJ
Fisher
M H
MH
Weber
A E
AE
D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004285:Dogs; D006801:Humans; D008253:Macaca mulatta; D008297:Male; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D022702:Receptors, Adrenergic, beta-3; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
D000318:Adrenergic beta-Agonists; C112650:L 755507; D011943:Receptors, Adrenergic, beta; D022702:Receptors, Adrenergic, beta-3; D013449:Sulfonamides