19 February 2024
Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system (CNS), exerting its effects via two classes of receptors, GABAA and GABAB. GABAA receptors (GABAARs) are ligand-gated ion channels typically composed of two alpha (alpha1–6), two beta (beta1–3), and one gamma (gamma1–3) or delta subunits. Genetic and pharmacological studies of GABAARs containing alpha5 subunits in particular, suggest these may play important roles in learning and memory processes, as a result of their high expression in the hippocampus and olfactory bulb.
Allosteric modulators can bind at the interface of alpha and beta subunits and while having no effect on their own, can increase (positive allosteric modulator or PAM) or decrease (negative allosteric modulator or NAM) the receptor’s activity in the presence of GABA. While most currently available NAMs do not show subtype selectivity and therefore act on all GABAARs, BI-1030 is functionally selective for the GABAA receptor subtypes alpha1, alpha2, and alpha3.
To enable further research into the functional role of alpha5 GABAARs, you can now order BI-1030 for free on opnMe. You will retain full ownership and control of your results, which we encourage you to publish.
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About BI-1030:
BI-1030 is a potent and functionally selective GABAA alpha5 receptor negative allosteric modulator, suitable for in vitro as well as in vivo use. Its favorable profile in different CNS in vivo models render it a reliable molecular tool to investigate the complex signaling mechanisms underlying synaptic plasticity, cognition and memory.
About opnMe:
opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. As part of our first pillar, the “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. These are complemented by “Molecules for Collaboration” where we offer access to unprecedented, often unpublished molecules, together with an attractive funding package. Interested scientists are invited to submit testable research hypotheses with these assets. With our “opn2EXPERTS” program, we enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs, such as our recent call on “unraveling the role of AGR2 in lung fibrosis”.