Literature DB >> 14667209

Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.

Xiaoyan Li1, Hui Cao, Chunchun Zhang, Roman Furtmueller, Karoline Fuchs, Sigismund Huck, Werner Sieghart, Jeffrey Deschamps, James M Cook.   

Abstract

The synthesis and in vitro affinity of the alpha5beta3gamma2 (alpha5) subtype selective BzR/GABA(A) antagonist 7 is described. This ligand is selective for alpha5 subtypes in vitro and is a potent antagonist of the effects of diazepam only at alpha5beta3gamma2 subtypes (oocytes). Ligands such as 7 will be important in the determination of which physiological function(s) are subserved by this GABA(A) alpha5 subtype.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 14667209     DOI： 10.1021/jm034164c

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  16 in total

1.  Cognition-impairing effects of benzodiazepine-type drugs: role of GABAA receptor subtypes in an executive function task in rhesus monkeys.

Authors:  Leah Makaron; Casey A Moran; Ojas Namjoshi; Sundari Rallapalli; James M Cook; James K Rowlett
Journal:  Pharmacol Biochem Behav       Date:  2013-01-02       Impact factor: 3.533

2.  Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.

Authors:  Wenyuan Yin; Samarpan Majumder; Terry Clayton; Steven Petrou; Michael L VanLinn; Ojas A Namjoshi; Chunrong Ma; Brett A Cromer; Bryan L Roth; Donna M Platt; James M Cook
Journal:  Bioorg Med Chem       Date:  2010-09-29       Impact factor: 3.641

3.  The role of α1 and α5 subunit-containing GABAA receptors in motor impairment induced by benzodiazepines in rats.

Authors:  Marija Milić; Jovana Divljaković; Sundari Rallapalli; Michael L van Linn; Tamara Timić; James M Cook; Miroslav M Savić
Journal:  Behav Pharmacol       Date:  2012-04       Impact factor: 2.293

4.  Subtype selectivity of α+β- site ligands of GABAA receptors: identification of the first highly specific positive modulators at α6β2/3γ2 receptors.

Authors:  Zdravko Varagic; Joachim Ramerstorfer; Shengming Huang; Sundari Rallapalli; Isabella Sarto-Jackson; James Cook; Werner Sieghart; Margot Ernst
Journal:  Br J Pharmacol       Date:  2013-05       Impact factor: 8.739

5.  α5-GABAA receptors negatively regulate MYC-amplified medulloblastoma growth.

Authors:  Soma Sengupta; Shyamal Dilhan Weeraratne; Hongyu Sun; Jillian Phallen; Sundari K Rallapalli; Natalia Teider; Bela Kosaras; Vladimir Amani; Jessica Pierre-Francois; Yujie Tang; Brian Nguyen; Furong Yu; Simone Schubert; Brianna Balansay; Dimitris Mathios; Mirna Lechpammer; Tenley C Archer; Phuoc Tran; Richard J Reimer; James M Cook; Michael Lim; Frances E Jensen; Scott L Pomeroy; Yoon-Jae Cho
Journal:  Acta Neuropathol       Date:  2013-11-07       Impact factor: 17.088

6.  Antagonism of triazolam self-administration in rhesus monkeys responding under a progressive-ratio schedule: In vivo apparent pA2 analysis.

Authors:  Bradford D Fischer; Donna M Platt; Sundari K Rallapalli; Ojas A Namjoshi; James M Cook; James K Rowlett
Journal:  Drug Alcohol Depend       Date:  2015-10-30       Impact factor: 4.492

7.  The differential role of alpha1- and alpha5-containing GABA(A) receptors in mediating diazepam effects on spontaneous locomotor activity and water-maze learning and memory in rats.

Authors:  Miroslav M Savić; Marija M Milinković; Sundari Rallapalli; Terry Clayton; Sroan Joksimović; Michael Van Linn; James M Cook
Journal:  Int J Neuropsychopharmacol       Date:  2009-03-06       Impact factor: 5.176

8.  A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.

Authors:  Dongmei Han; F Holger Försterling; Xiaoyan Li; Jeffrey R Deschamps; Damon Parrish; Hui Cao; Sundari Rallapalli; Terry Clayton; Yun Teng; Samarpan Majumder; Subramaniam Sankar; Bryan L Roth; Werner Sieghart; Roman Furtmuller; James K Rowlett; Michael R Weed; James M Cook
Journal:  Bioorg Med Chem       Date:  2008-09-02       Impact factor: 3.641

9.  Modulation of α5 subunit-containing GABAA receptors alters alcohol drinking by rhesus monkeys.

Authors:  Daniela Rüedi-Bettschen; James K Rowlett; Sundari Rallapalli; Terry Clayton; James M Cook; Donna M Platt
Journal:  Alcohol Clin Exp Res       Date:  2012-11-05       Impact factor: 3.455

10.  Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.

Authors:  Michaela Jansen; Holger Rabe; Axelle Strehle; Sandra Dieler; Fabian Debus; Gerd Dannhardt; Myles H Akabas; Hartmut Lüddens
Journal:  J Med Chem       Date:  2008-07-24       Impact factor: 7.446
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.