|Description||MK 0343, also known as MRK-409, is a subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively). MK-0343 is a non-sedating anxiolytic in preclinical species but causes sedation in humans.|
|Synonyms||7-cyclobutyl-3-(2,6-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine; MK-0343; MK 0343; MK0343; MRK 409; MRK409; MRK-409|
Org 20599 is an anaesthetic steroid. It has modulatory effects on GABAA receptors. Org 20599 is a potential theraputic for migraines and headaches.
This active molecular is a highly selective inverse agonist/negative allosteric modulator GABAAα5 receptors. It was developed by Roche to treat cognitive impair...
TACA, the trans-isomer of CACA, is a potent GABAA and GABAC agonist, GABA uptake inhibitor and substrate for GABA-T. It also acts as a GABAA-ρ agonist.
(-)-Bicuculline methiodide is the methiodide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.
FG 7142 is a benzodiazepine inverse agonist and anxiogenic agent. FG 7142 increases tyrosine hydroxylation and upregulates β-adrenoceptors in mouse cerebral cor...
Bretazenil is a partial agonist at the GABAA benzodiazepine site (EC50 = 10 nM at α1β1γ2 receptors) that potentiates GABA responses on α4β3γ2 cells. Bretazenil ...
SKF 97541 is a highly potent GABAB agonist, and also acts as a GABAA-ρ antagonist. SKF 97541 exhibits sedative effects in mammals and has the potential to be us...
RuBi-GABA, a ruthenium-bipyridine-triphenylphosphine caged GABA, is a photolabile protecting group used for highly efficient visible light GABA uncaging.
Phaclofen, a phosphonic acid derivative of Baclofen, is a selective GABAB antagonist.
NNC 05-2090 hydrochloride
NNC052090 is a GABA uptake inhibitor that displays selectivity for BGT-1 (mGAT-2) transporters.
FGIN-1-43 is a potent and specific ligand for the mitochondial DBI receptor (MDR).
Indiplon acts as a high-affinity positive and orally active allosteric modulator of the GABAA receptor (Ki=1.2 nM in rat frontal cortex and Ki=1.7 nM and in cer...
NNC 711 is a GABA uptake inhibitor by GAT-1 with IC50 values of 0.04, 171, 1700 and 622 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1. NNC 711 is an anticonvulsantag...
Pregnanolone, also known as Kabi-2213, SKF 6455, Eltanolone, is a GABAA receptor positive allosteric modulator potentially for the treatment of pain.
(-)-Bicuculline methochloride is the methochloride salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.
Etomidate is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
Afloqualone is a agonist of GABA receptor has sedative and muscle-relaxant effects.
ZK 93423 hydrochloride
ZK 93423 hydrochloride is a potent and non-selective benzodiazepine receptor agonist (IC50 = 1 nM) (Ki = 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 ...
Ganaxolone is a positive allosteric modulator of GABAA receptors with anticonvulsive anxiolytic properties. Ganaxolone enhances GABA-evoked chloride currents in...
Pagoclone, an active (+)-enantiomer of the racemate RP 59037, is a ubtype selective partial agonist at GABAA receptor and used for the treatment of panic and an...