Author/Authors :
Mary Chebib، نويسنده , , Graham A. R. Johnston، نويسنده , , Jan P. Mattsson، نويسنده , , Karin Rydstr?m، نويسنده , , Karolina Nilsson، نويسنده , , Jian Qiu، نويسنده , , Scott H. Stevenson، نويسنده , , Richard B. Silverman، نويسنده ,
Abstract :
3- and 4-(Aminomethyl)-2,6-difluorophenols were tested for activity against the three major classes of GABA receptors. 4-(Aminomethyl)-2,6-difluorophenol was shown to be a competitive and somewhat selective antagonist at 1 GABAC receptors expressed in Xenopus oocytes (KB = 75.5 μM with a 95% Confidence Interval range of 75.2 μM to 75.8 μM). This is the first in a novel class of increased lipophilicity GABAC receptor antagonists with little activity at α1β2γ2 GABAA and GABAB receptors.
