| Cat. No. |
Product Name |
Information |
| PC-63442 |
ONO-8590580
GABAA α5 PAM
|
ONO-8590580 is a novel potent, selective GABAA α5 negative allosteric modulator, binds to the benzodiazepine binding sites on recombinant human α5-containing GABAA receptors with Ki of 7.9 nM. |
| PC-63310 |
MIDD0301
α5β3γ2 GABAA inhibitor
|
MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM. |
| PC-63159 |
AZD3043
GABAA PAM
|
AZD 3043 (THRX-918661) is a positive allosteric modulator of the GABAA receptor in vitro and a sedative/hypnotic agent in vivo, potentiates GABAA receptor-mediated chloride currents with EC50 of 36 uM. |
| PC-62772 |
MRK-696
GABAA α2/α3 agonist
|
MRK-696 is a non-selective benzodiazepine receptor partial agonist, functional selectivity for α2/α3 subunit-containing GABAA receptors. |
| PC-62771 |
TP003
GABAA α3 agonist
|
TP003 is a potent, functional selectivity for α3 subunit-containing GABAA receptor agonist with Ki of <1 nM for α1β3γ2, α2β3γ2, α3β3γ2 and α5β3γ2, has no affinity for α4β3γ2 and α6β3γ2 (Ki>1 uM). |
| PC-62770 |
MRK-623
GABAA α2/α3 agonist
|
MRK-623 is a potent, α2/α3 subunit functionally selectivie GABAA receptor agonist with Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. |
| PC-62769 |
TPA023
GABAA α2/α3 agonist
|
TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors. |
| PC-62768 |
TPA023B
GABAA α2/α3 agonist
|
TPA023B is a potent, α2/α3 subtype-selective GABAA receptor partial agonist with Ki of 2.0 and 1.8 nM, does not affect the functioning of the α1 subtype. |
| PC-62765 |
AZD6280
GABAA α2/α3 modulator
|
AZD6280 is a potent, α2/3 functionally selective, partial GABAA receptor modulator with pKi of 7.7. |
| PC-62764 |
Lesogaberan
GABAB agonist
|
Lesogaberan (AZD-3355) is a potent, selective, peripherally acting GABAB receptor agonist with Ki of 5 nM and EC50 of 8.6 nM, 274-fold selectivity over GABAA (Ki=1.4 uM). |
| PC-62759 |
CPP-115
GABA aminotransferase inhibitor
|
CPP-115 is an orally available, small molecule, next-generation GABA aminotransferase (GABA-AT) inhibitor with Ki of 31 uM, without other GABAergic or off-target activities. |
| PC-62625 |
PWZ-029
α5-GABAAR inverse agonist
|
PWZ-029 is a potent, subtype-selective partial inverse agonist of α5 GABAA receptors with Ki of 30 nM, demonstrates memory enhancing effects in vivo. |
