Table 1.
Summary table of α5 subunit containing GABA type A receptor (α5 GABAAR) targeted drugs and potential utility.
| Drug type | Reduce α5 GABAAR activity (NAM or competetive antagonist) | Increase α5 GABAAR activity (PAM) |
|---|---|---|
| Compound | L-655, 708, α5IA, Ro15-4513, MRK-016, RO4938581, RY-80, S44819 (competetive antagonist) | SH-053-R-CH3-2′F, MP-III-022, Compound 44, GL-II-73 |
| Therapeutic potential | Procognition/smart drugs | Mild cognitive impairment in aging |
| Neurodevelopmental disorders with excessive GABAergic neurotransmission | Neurodevelopmental disorders with insufficient inhibitory tone | |
| Inflammation induced mild cognitive impairment | Depression | |
| Post-anesthesia memory blockade | Schizophrenia |
This includes drugs that can reduce α5 GABAAR activity [negative allosteric modulators (NAMs) and the competitive antagonist S44819] and positive allosteric modulators (PAMs) that enhance α5 GABAAR activity. Representative compounds and therapeutic potential are listed.