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Items: 1 to 20 of 102

1.

Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands.

Richter L, de Graaf C, Sieghart W, Varagic Z, Mörzinger M, de Esch IJ, Ecker GF, Ernst M.

Nat Chem Biol. 2012 Mar 25;8(5):455-64. doi: 10.1038/nchembio.917.

2.

Relative positioning of diazepam in the benzodiazepine-binding-pocket of GABA receptors.

Tan KR, Baur R, Charon S, Goeldner M, Sigel E.

J Neurochem. 2009 Dec;111(5):1264-73. doi: 10.1111/j.1471-4159.2009.06419.x. Epub 2009 Oct 5.

3.

Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents.

Salerno S, Da Settimo F, Taliani S, Simorini F, La Motta C, Fornaciari G, Marini AM.

Curr Top Med Chem. 2012;12(4):286-311. Review.

PMID:
22204484
4.

Discovery of anxiolytic 2-ferrocenyl-1,3-thiazolidin-4-ones exerting GABAA receptor interaction via the benzodiazepine-binding site.

Pejović A, Denić MS, Stevanović D, Damljanović I, Vukićević M, Kostova K, Tavlinova-Kirilova M, Randjelović P, Stojanović NM, Bogdanović GA, Blagojević P, D'hooghe M, Radulović NS, Vukićević RD.

Eur J Med Chem. 2014 Aug 18;83:57-73. doi: 10.1016/j.ejmech.2014.05.062. Epub 2014 May 28.

PMID:
24950490
5.

Ligands for the benzodiazepine binding site--a survey.

Teuber L, Wätjens F, Jensen LH.

Curr Pharm Des. 1999 May;5(5):317-43. Review.

PMID:
10213798
6.

On the benzodiazepine binding pocket in GABAA receptors.

Berezhnoy D, Nyfeler Y, Gonthier A, Schwob H, Goeldner M, Sigel E.

J Biol Chem. 2004 Jan 30;279(5):3160-8. Epub 2003 Nov 11.

7.
8.

Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives.

Faizi M, Dabirian S, Tajali H, Ahmadi F, Zavareh ER, Shahhosseini S, Tabatabai SA.

Bioorg Med Chem. 2015 Feb 1;23(3):480-7. doi: 10.1016/j.bmc.2014.12.016. Epub 2014 Dec 19.

PMID:
25564376
9.
10.

Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: the approximated activation of receptor subtypes may explain behavioral effects.

Obradović ALj, Joksimović S, Poe MM, Ramerstorfer J, Varagic Z, Namjoshi O, Batinić B, Radulović T, Marković B, Roth BL, Sieghart W, Cook JM, Savić MM.

Brain Res. 2014 Mar 20;1554:36-48. doi: 10.1016/j.brainres.2014.01.036. Epub 2014 Jan 25.

12.
13.

The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes.

Ramerstorfer J, Furtmüller R, Vogel E, Huck S, Sieghart W.

Eur J Pharmacol. 2010 Jun 25;636(1-3):18-27. doi: 10.1016/j.ejphar.2010.03.015. Epub 2010 Mar 19.

PMID:
20303942
14.

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.

McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR, Farrar S, Myers J, Cook G, Ferris P, Garrett L, Bristow L, Marshall G, Macaulay A, Brown N, Howell O, Moore KW, Carling RW, Street LJ, Castro JL, Ragan CI, Dawson GR, Whiting PJ.

Nat Neurosci. 2000 Jun;3(6):587-92.

PMID:
10816315
16.

Relative positioning of classical benzodiazepines to the γ2-subunit of GABAA receptors.

Middendorp SJ, Hurni E, Schönberger M, Stein M, Pangerl M, Trauner D, Sigel E.

ACS Chem Biol. 2014 Aug 15;9(8):1846-53. doi: 10.1021/cb500186a. Epub 2014 Jul 1.

PMID:
24918742
17.

Geometrically constrained derivatives of indolylglyoxylamides as ligands binding the GABAA/BzR complex.

Sartini S, Morelli M, Simorini F, Taliani S, Salerno S, Marini AM, Da Settimo F, La Motta C.

Curr Top Med Chem. 2012;12(4):312-20. Review.

PMID:
22204489
18.

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.

Hintermann S, Hurth K, Nozulak J, Tintelnot-Blomley M, Aichholz R, Blanz J, Kaupmann K, Mosbacher J.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1523-6. doi: 10.1016/j.bmcl.2010.12.107. Epub 2010 Dec 28.

PMID:
21277199
19.

Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes.

Rudolph U, Crestani F, Benke D, Brünig I, Benson JA, Fritschy JM, Martin JR, Bluethmann H, Möhler H.

Nature. 1999 Oct 21;401(6755):796-800. Erratum in: Nature 2000 Apr 6;404(6778):629.

PMID:
10548105
20.

Recent developments in potential anxiolytic agents targeting GABAA/BzR complex or the translocator protein (18kDa) (TSPO).

Nothdurfter C, Rupprecht R, Rammes G.

Curr Top Med Chem. 2012;12(4):360-70. Review.

PMID:
22204486
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