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

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.

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6,3′-Dibromoflavone and 6-Nitro-3′-bromoflavone: New Additions to the 6,3′-Disubstituted Flavone Family of High-Affinity Ligands of the Brain Benzodiazepine Binding Site with Agonistic Properties

Biochemical and Biophysical Research Communications ◽

10.1006/bbrc.2000.2979 ◽

2000 ◽

Vol 273 (2) ◽

pp. 694-698 ◽

Cited By ~ 13

Author(s):

Haydee Viola ◽

Mariel Marder ◽

Cristina Wasowski ◽

Osvaldo Giorgi ◽

Alejandro C. Paladini ◽

...

Keyword(s):

Binding Site ◽

Affinity Ligands ◽

High Affinity ◽

Benzodiazepine Binding ◽

The Brain

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The peripheral high affinity benzodiazepine binding site is not coupled to the cardiac Ca2+ channel

European Journal of Pharmacology ◽

10.1016/0014-2999(85)90140-2 ◽

1985 ◽

Vol 118 (3) ◽

pp. 293-301 ◽

Cited By ~ 39

Author(s):

Mark Holck ◽

Wolfgang Osterrieder

Keyword(s):

Binding Site ◽

High Affinity ◽

Benzodiazepine Binding

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

Journal of Medicinal Chemistry ◽

10.1021/jm00001a005 ◽

1995 ◽

Vol 38 (1) ◽

pp. 16-20 ◽

Cited By ~ 47

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

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ChemInform Abstract: 5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl) -7-phenyl-2,3,6,7-tetrahydro-1,4-thiazepines as Compounds with High Affinity at the Benzodiazepine Binding Site on GABAA Receptors.

ChemInform ◽

10.1002/chin.201125210 ◽

2011 ◽

Vol 42 (25) ◽

pp. no-no

Author(s):

C. Grunwald ◽

C. Kronbach ◽

U. Egerland ◽

R. Schindler ◽

R. Dieckmann ◽

...

Keyword(s):

Binding Site ◽

Gabaa Receptors ◽

High Affinity ◽

Benzodiazepine Binding

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Zolpidem dependence with frontal lobe syndrome: a case report

International Journal of Basic & Clinical Pharmacology ◽

10.18203/2319-2003.ijbcp20175222 ◽

2017 ◽

Vol 6 (12) ◽

pp. 2936 ◽

Cited By ~ 1

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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