Title of article
Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABAC receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 1999
Pages
6
From page
3093
To page
3098
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1999
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790486
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