1区 · 医学
Article
作者: Wensink, Erica J. ; Strakhova, Marina I. ; Altenbach, Robert J. ; Garrison, Tiffany Runyan ; Brioni, Jorge D. ; Wetter, Jill M. ; Cowart, Marlon D. ; Hsieh, Gin C. ; Manelli, Arlene M. ; Honore, Prisca ; Carr, Tracy L. ; Marsh, Kennan C. ; Black, Lawrence A.
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.