Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors

2021 ◽  
Author(s):  
Frederik Rostrup ◽  
Christina B. Falk-Petersen ◽  
Kasper Harpso̷e ◽  
Stine Buchleithner ◽  
Irene Conforti ◽  
...  
Keyword(s):  
Mode Of Action ◽  
Type A ◽  
Aminobutyric Acid ◽  
Structural Determinants ◽  
Acid Type

scholarly journals Structural Determinants for the Mode of Action of the Imidazopyridine DS2 at d-containing g-Aminobutyric Acid Type A (GABAA) Receptors

2020 ◽  
Author(s):  
Bente Frølund ◽  
Frederik Rostrup ◽  
Christina Birkedahl Falk-Petersen ◽  
Kasper Harpsøe ◽  
Stine Buchleithner ◽  
...  
Keyword(s):  
Membrane Potential ◽  
Gabaa Receptors ◽  
Mode Of Action ◽  
Aminobutyric Acid ◽  
Functional Assay ◽  
Pharmacological Profile ◽  
Structural Determinants ◽  
Acid Type ◽  
Plate Reader ◽  
Sar Study

<div>A SAR study of the delta-selective positive modulators DS2 was performed to assist the quest for the binding site. The modulatory effect was measured using a fluorometric inaging plate reader (FLIPR) membrane potential (FMP) functional assay. Specific positions in the structural scaffold of DS2 was found to severly affect the pharmacological profile. <br></div><div>Analogs superior to DS2 were identified displaying higher potency and selectivity for the alfa4beta1delta over alfa4beta1gamma.<br></div><br>

scholarly journals Structural Determinants for the Mode of Action of the Imidazopyridine DS2 at d-containing g-Aminobutyric Acid Type A (GABAA) Receptors

2020 ◽  
Author(s):  
Bente Frølund ◽  
Frederik Rostrup ◽  
Christina Birkedahl Falk-Petersen ◽  
Kasper Harpsøe ◽  
Stine Buchleithner ◽  
...  
Keyword(s):  
Membrane Potential ◽  
Gabaa Receptors ◽  
Mode Of Action ◽  
Aminobutyric Acid ◽  
Functional Assay ◽  
Pharmacological Profile ◽  
Structural Determinants ◽  
Acid Type ◽  
Plate Reader ◽  
Sar Study

<div>A SAR study of the delta-selective positive modulators DS2 was performed to assist the quest for the binding site. The modulatory effect was measured using a fluorometric inaging plate reader (FLIPR) membrane potential (FMP) functional assay. Specific positions in the structural scaffold of DS2 was found to severly affect the pharmacological profile. <br></div><div>Analogs superior to DS2 were identified displaying higher potency and selectivity for the alfa4beta1delta over alfa4beta1gamma.<br></div><br>

[11C]Flumazenil Positron Emission Tomography Analyses of Brain Gamma-Aminobutyric Acid Type A Receptors in Angelman Syndrome

2008 ◽  
Vol 152 (4) ◽  
pp. 546-549.e3 ◽  
Author(s):  
Naoko Asahina ◽  
Tohru Shiga ◽  
Kiyoshi Egawa ◽  
Hideaki Shiraishi ◽  
Shinobu Kohsaka ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Angelman Syndrome ◽  
Type A ◽  
Emission Tomography ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Positron Emission ◽  
Acid Type
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