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ePoster
BI-1030 IS A NEGATIVE ALLOSTERIC MODULATOR (NAM) OF GABAA Α5-CONTAINING RECEPTORS
Sarah Streicherand 7 co-authors
Boehringer Ingelheim Pharma GmbH & Co. KG
FENS Forum 2026 (2026)
Barcelona, Spain
Board PS01-07AM-486
Presentation
Date TBA
Board: PS01-07AM-486
Event Information
Poster Board
PS01-07AM-486
Poster
View posterAbstract
Gamma-aminobutyric type A receptors (GABAARs) are ligand-gated chloride channels with a heteropentameric structure that is composed of two alpha (alpha 1-6), two beta (beta 1-3) and one gamma (gamma 1-3) or delta subunit1,2. Upon GABA binding, the channel opens, allowing chloride ion flux that mediates inhibitory neurotransmission. Dysfunction of these receptors has been implicated in several neurological disorders, including schizophrenia, autism, and epilepsy3,4,5, with predominant expression in the hippocampus. Notably, GABAA KO mice exhibit enhanced learning and memory6, highlighting the potential of a α5 NAM as a cognitive enhancer in schizophrenia. Our selective and in-vivo ready α5 NAM has a mode of action well-suited for targeting the extrasynaptic α5-containing GABA receptors. The compound is available to the scientific community via the opnMe.com platform for further research and exploration7.
- Sigel, E. & Steinmann, M.E., J. Biol. Chem. 2012, 287, 40224
- Olsen, R. W. & Sieghart, W., Neuropharmacology, 2009, 56, 141
- Braat, S. & Kooy, R.F. Neuron, 2015, 86, 1119
- Macdonald, R.L., Kang, J.-Q. & Gallagher, M.J., J. Physiol., 2010, 588, 1861
- Jacob, T.C., Front.Mol. Neurosci. 2019, 12: 179
- Collinson et al. (2002) J.Neurosci. 22(13): 5572-5580
- opnMe.com Boehringer Ingelheim (2017): opnMe - Boehringer Ingelheim Open Innovation Portal.
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