scholarly journals Identifying the Propofol Binding Site(S) in Heterologously Expressed Human Alpha1 Beta3 Gaba-A Receptors using a Photoreactive Propofol Analog

2013 ◽  
Vol 104 (2) ◽  
pp. 637a ◽  
Author(s):  
Selwyn S. Jayakar ◽  
Xiaojuan Zhou ◽  
Zuzana Dostalova ◽  
William P. Dailey ◽  
Keith W. Miller ◽  
...  
Keyword(s):  
Binding Site ◽  
Gaba A

scholarly journals The Binding Site of TETS in the Pore of the α2B3γ2L Gaba-A Receptor

2020 ◽  
Vol 118 (3) ◽  
pp. 580a
Author(s):  
Brandon Pressly ◽  
Heike Wulff ◽  
Ruth Lee
Keyword(s):  
Binding Site ◽  
Gaba A

scholarly journals Binding site location on GABA A receptors determines whether mixtures of intravenous general anaesthetics interact synergistically or additively in vivo

2019 ◽  
Vol 176 (24) ◽  
pp. 4760-4772 ◽  
Author(s):  
Daniel E. Kent ◽  
Pavel Y. Savechenkov ◽  
Karol S. Bruzik ◽  
Keith W. Miller
Keyword(s):  
Binding Site ◽  
Site Location ◽  
Gaba A

scholarly journals A Single Steroid-binding Site is Sufficient for Potentiation of GABA-A Receptors

2009 ◽  
Vol 96 (3) ◽  
pp. 487a
Author(s):  
Joe Henry Steinbach ◽  
John R. Bracamontes
Keyword(s):  
Binding Site ◽  
Gaba A ◽  
Steroid Binding

scholarly journals Prediction of the Anxiolytic Action Mediated by the GABA A Receptor by the Molecular Docking Method

2020 ◽  
Vol 6 (5) ◽  
pp. 38-45
Author(s):  
T. Gendugov ◽  
A. Glushko ◽  
A. Chiriapkin ◽  
V. Chiriapkin
Keyword(s):  
Amino Acids ◽  
Molecular Docking ◽  
Binding Site ◽  
Computational Experiment ◽  
Gaba A ◽  
High Affinity ◽  
Docking Method ◽  
Benzodiazepine Binding ◽  
Docking Energy ◽  
Molecular Docking Method

The article considers the study in silico of the affinity of 3-[2-oxo-2-(4-phenyl-1-piperazinyl)ethyl]-4(3H)-quinazolinone (VMA-10-21 compound) to the benzodiazepine binding site of the GABA А receptor by molecular docking method. The computational experiment was carried out using a set of Autodock programs. As a result, the method for predicting the affinity of the simulated compounds to the benzodiazepine binding site of the GABA A receptor was developed. The highest correlation coefficient between the pKi value and the average docking energy in the benzodiazepine binding site (0.54) was obtained using a set of amino acids Tyr 58 and Tyr 159. The predicted Ki value of the VMA-10-21 compound is 2.864 nM, which suggests a high affinity of the studied compound to this receptor.

scholarly journals Pharmacological Selectivity of a Steroid Binding Site at the Beta+-Alpha− Interface of Alpha1 Beta3 Gaba-A Receptors

2019 ◽  
Vol 116 (3) ◽  
pp. 392a
Author(s):  
Selwyn S. Jayakar ◽  
Xiaojuan Zhou ◽  
Bo Wu ◽  
Keith W. Miller ◽  
Karol S. Bruzik ◽  
...  
Keyword(s):  
Binding Site ◽  
Gaba A ◽  
Steroid Binding

Potential Anxiolytic Agents. Pyrido[1,2-a]benzimidazoles: A New Structural Class of Ligands for the Benzodiazepine Binding Site on GABA-A Receptors

1995 ◽  
Vol 38 (1) ◽  
pp. 16-20 ◽  
Author(s):  
Bruce E. Maryanoff ◽  
Winston Ho ◽  
David F. McComsey ◽  
Allen B. Reitz ◽  
Philip P. Grous ◽  
...  
Keyword(s):  
Binding Site ◽  
Structural Class ◽  
Gaba A ◽  
Benzodiazepine Binding

scholarly journals Comparing the high affinity benzodiazepine binding site with the homologous “CGS 9895” site in GABA‐A receptors (1059.1)

2014 ◽  
Vol 28 (S1) ◽  
Author(s):  
Roshan Puthenkalam ◽  
Zdravko Varagic ◽  
Anna Dereky ◽  
Chonticha Suwattanasophon ◽  
Isabella Sarto‐Jackson ◽  
...  
Keyword(s):  
Binding Site ◽  
Gaba A ◽  
High Affinity ◽  
Benzodiazepine Binding ◽  
Cgs 9895

scholarly journals Methylene blue inhibits GABA A receptors by interaction with GABA binding site

2017 ◽  
Vol 119 ◽  
pp. 100-110 ◽  
Author(s):  
Zhenglan Chen ◽  
Ran Liu ◽  
Shao-Hua Yang ◽  
Glenn H. Dillon ◽  
Renqi Huang
Keyword(s):  
Methylene Blue ◽  
Binding Site ◽  
Gaba A ◽  
Gaba Binding

scholarly journals Positional clustering improves computational binding site detection and identifies novel cis -regulatory sites in mammalian GABA A receptor subunit genes

2007 ◽  
Vol 35 (3) ◽  
pp. e20-e20 ◽  
Author(s):  
Timothy E. Reddy ◽  
Boris E. Shakhnovich ◽  
Daniel S. Roberts ◽  
Shelley J. Russek ◽  
Charles DeLisi
Keyword(s):  
Binding Site ◽  
Receptor Subunit ◽  
Gaba A ◽  
Regulatory Sites

scholarly journals Zolpidem dependence with frontal lobe syndrome: a case report

2017 ◽  
Vol 6 (12) ◽  
pp. 2936 ◽  
Author(s):  
Udayan Majumder ◽  
Rajesh Das ◽  
Rajkumar Lenin Singh
Keyword(s):  
Case Report ◽  
Side Effects ◽  
Binding Site ◽  
Efficacy And Safety ◽  
Short Term ◽  
Gaba A ◽  
Acid Type ◽  
Benzodiazepine Binding ◽  
Term Basis ◽  
Frontal Lobe Syndrome

Zolpidem is a non-benzodiazepine sedative hypnotic that binds to the benzodiazepine binding site on the gammaaminobutyric acid type A (GABA-A) receptors. It is the most commonly prescribed sleep medication which has been shown to be effective for treating insomnia on a short-term basis with fewer side effects than traditional benzodiazepines, which are feared for their abuse and dependence potential. Many studies have reported efficacy and safety of zolpidem in treatment of insomnia keeping in mind about its low abuse, and dependence capability. We present a case of zolpidem dependence in a 36-year-old male to emphasize that zolpidem also should be judiciously prescribed under supervision so that it does not develop tolerance, abuse and dependence.

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