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RO4938581
- Development stage
- Discontinued
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
RO4938581 is a potent, selective, brain-penetrant small molecule negative allosteric modulator (inverse agonist) of the GABAA receptor containing the alpha5 subunit (GABRA5). Originally developed by Hoffmann-La Roche as a cognitive enhancer (nootropic) for the potential treatment of cognitive dysfunctions (such as those associated with Down syndrome, schizophrenia, or aging), it exhibits high binding and functional selectivity for the alpha5 subunit over alpha1, alpha2, and alpha3 subunits. This selectivity avoids the anxiogenic and pro-convulsant side effects typically associated with non-selective GABAA receptor inverse agonists. Although selected as a clinical candidate, its development was halted preclinically (reportedly due to hepatotoxicity), and it is now widely used as an open-access chemical probe distributed by the Structural Genomics Consortium (SGC) in collaboration with Pfizer.
- Other names
- Ro 4938581Ro4938581Ro-4938581
02
Targets
α5-GABAAR (Gamma-aminobutyric acid type A receptor alpha5beta2gamma2 subtype (GABAA receptor alpha5beta2gamma2 subtype))GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)
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