Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Compounds with various activities and selectivities were discovered through structure-activity relationship studies of bicifadine analogs as monoamine transporter inhibitors. The norepinephrine-selective 2-thienyl compound S-6j was efficacious in a rodent pain model.
Zhang
Mingzhu
M
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Jovic
Florence
F
Vickers
Troy
T
Dyck
Brian
B
Tamiya
Junko
J
Grey
Jonathan
J
Tran
Joe A
JA
Fleck
Beth A
BA
Pick
Rebecca
R
Foster
Alan C
AC
Chen
Chen
C
D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry* / Q000494:pharmacology*; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D026901:Membrane Transport Proteins / Q000737:chemistry / Q000494:pharmacology; D008956:Models, Chemical; D018377:Neurotransmitter Agents / Q000378:metabolism; D050479:Neurotransmitter Transport Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry*; D009638:Norepinephrine / Q000737:chemistry; D010146:Pain; D051381:Rats; D013329:Structure-Activity Relationship
D019086:Bridged Bicyclo Compounds, Heterocyclic; D026901:Membrane Transport Proteins; D018377:Neurotransmitter Agents; D050479:Neurotransmitter Transport Proteins; C034438:bicifadine; D009638:Norepinephrine