|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|
CP-457920, also called as NGD 971, is a selective α5 GABAA receptor inverse agonist (Ki of ~ 1 ng/mL). CP-457920 was progressed into clinical studies for the tr...
Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
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...
CGP52432 is a potent and selective GABAB receptor antagonist with IC50 value of 85 nM.
CH-50911 is a selective GABA-B antagonist with IC50 value of 1.1 μM. It is developed by Schering-Plough Corporation. CH-50911 is often used in pharmacology rese...
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...
Arbaclofen placarbil is a prodrug of R-baclofen. It is a GABA B receptor agonist. Arbaclofen was being developed as a potential treatment for patients with GERD...
CI966 is a highly potent and selective blocker of the GABA transporter 1 (GAT-1) with IC50 value of 0.26 µM acting as a central nervous system depressant. It ha...
Etifoxine Hydrochloride is Potentiator of GABAA receptor with anxiolytic and anticonvulsant activity.
Cardiazole is a GABA(A) receptor antagonist, causes alterations in excitatory and inhibitory neurotransmitter systems.
Gaboxadol is a GABA agonist. It was a non-opioid analgesic and a novel type of hypnotic. It was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-...
Isoguvacine hydrochloride is a selective GABA receptor agonist with anticonvulsant and antiepileptic effect, developed for Neuroscience research.
Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions.
Progabide is a gamma-aminobutyric acid (GABA) antagonist. It has agonistic activity for both the GABAA and GABAB receptors. It has antiepileptic activity and is...
L-DABA, (L-2,4-Diaminobutyric acid) is a noncompetitive GABA transaminase inhibitor (IC50> 500 μM) with antitumor activity in vivo and in vitro.
Acamprosate calcium is a gamma-aminobutyric acid(GABA)agonist and modulator of glutamatergic systems. It has been used in alcohol dependence treatments and may ...
NS 11394 is a drug with selectivity for the α3 and α5 subtypes. It acts as a subtype-selective positive allosteric modulator at GABAA receptors. It is used as a...
(R)-baclofen a selective GABAB agonist.
U 93631 is a ligand at the picrotoxin site of GABA(A) receptors, allosterically antagonizing GABA-induced Cl- currents. U-93631 causes rapid decay of gamma-amin...
Afloqualone is a agonist of GABA receptor has sedative and muscle-relaxant effects.