【文章名】Diaryldiamines with Dual Inhibition of the Histamine H-3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain
Diaryldiamines with Dual Inhibition of the Histamine H-3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain
作者
ALTENBACH ROBERT J; BLACK LAWRENCE A; STRAKHOVA MARINA I; MANELLI ARLENE M; CARR TRACY L; MARSH KENNAN C; WETTER JILL M; WENSINK ERICA J; HSIEH GIN C; HONORE PRISCA; GARRISON TIFFANY RUNYAN; BRIONI JORGE D; COWART MARLON D
[摘要]:A series of compounds was designed as dual inhibitors of the H-3 receptor and the norepinephrine transporter. Compound 5 (rNET K-i = 14 nM; rH(3)R K-i = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.