Table 2.
Summary of novel GABAA receptor subtype selective compounds.
| Target | Name | Efficacy (compared to a classical benzodiazepine) |
Affinity/Remarks | Ref |
|---|---|---|---|---|
| α 1 | Zolpidem | Comparable at α 1/α 2/α 3/α 5 | 5-10-fold higher affinity for α 1 versus α 2/3 > 1000 fold higher affinity for α 1 versus α 5 | [15] |
| α 2/3 | TPA023 | α 1 (0%), α 2 (11%), α 3 (21%), α 5 (5%) | Equivalent affinity | [8] |
| α 2/3 | TPA123 | α 1 (23%), α 2 (35%), α 3 (43%), α 5 (19%) | Equivalent affinity. Reinforcing efficacy and physiological dependence remained present | [8] |
| α 2/3 | L838,417 | α 1 (1.5%), α 2 (43%), α 3 (43%), α 5 (39%) | Equivalent affinity | [23] |
| α 2/3 | SL651498 |
α
1 (45%), α
2 (115%), α
3 (83%), α
5 (50%) Compared to zolpidem for α 1 efficacy |
5–10-fold increased affinity for α 2/3, 10–20 fold lower affinity for α 5 | [31] |