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RO5186582 + midazolam
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
RO5186582 + midazolam is a combination of an investigational, highly selective GABAA-α5 negative allosteric modulator (RO5186582, also known as basmisanil or RG1662), and midazolam, a short-acting benzodiazepine. RO5186582/basmisanil is under development as a cognition-enhancing agent, particularly for Down syndrome, acting by selectively reducing GABAergic inhibition at α5-containing GABAA receptors, which is believed to alleviate cognitive deficits by modulating inhibitory neurotransmission. Midazolam enhances GABAergic transmission via positive allosteric modulation of GABAA receptors, producing sedation, anxiolysis, muscle relaxation, anticonvulsant, and amnesic effects. Studies combining RO5186582 with midazolam have assessed drug-drug interactions, particularly regarding CYP3A4 metabolism and the pharmacodynamic effects on cognitive processes[4][7][9][10].
- Brand names
- BuccolamBusulfexNayzilamSeizalam
- Other names
- RO5186582RO-5186582RO 5186582basmisanilRG1662RG-1662RG 1662midazolam
02
Targets
BZD site (GABA-A receptor benzodiazepine site)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)
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