|Description||(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.|
PHP 501 trifluoroacetate
PHP 501 trifluoroacetate is potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells), with...
An agonist of an allosteric binding site on the GABA Receptor subtype A
(S)-(-)-4-Amino-2-hydroxybutyric acid is an analogue of γ-aminobutyric acid (GABA) that exhibits potential inhibitory activity on GABA binding and uptake by bra...
(-)-Bicuculline methiodide is the methiodide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.
Baclofen, an agonist of GABAB receptor, could be effective as a skeletal muscle relaxant and has been also found to have antispastic effect.
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-...
AA 29504 is a positive allosteric modulator of GABAA receptors with anxiolytic activity. It modulates both α4β3δ-containing extrasynaptic receptors and α1β3γ2S-...
BAR-501, a UDCA derivative, is a selective GPBAR1 agonist devoid of any FXR agonistic activity. BAR-501 effectively transactivates GPBAR1 in HEK293 cells overex...
Acamprosate calcium is a gamma-aminobutyric acid(GABA)agonist and modulator of glutamatergic systems. It has been used in alcohol dependence treatments and may ...
(R)-baclofen a selective GABAB agonist.
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...
(±)-Nipecotic acid is a nonselective GAT inhibitor that also induces GABA release through a process termed 'heteroexchange. IC50 = 8, 38, 106 and 2370 μM for hG...
TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand that acts as an agonist at α2 and antagonist at α1 benzodiazepine receptors (Ki = 118 and 245 nM, respe...
TPA023, also called as MK-0777, is a subtype-selective, mixed agonist-antagonist at GABAA receptor with anxiolytic and anticonvulsant effects.
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...
SL 651498 is a GABAA agonist selectively for subtype α2, and has the potential for the treatment of anxiety.
Isoguvacine hydrochloride is a selective GABA receptor agonist with anticonvulsant and antiepileptic effect, developed for Neuroscience research.
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...
Phaclofen, a phosphonic acid derivative of Baclofen, is a selective GABAB antagonist.
Loreclezole hydrochloride is a subtype-selective GABAA receptor modulator. It acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.