| DC8099 |
Saclofen
Featured
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Saclofen is a selective GABAB antagonist. |
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| DC10651 |
SSD114 hydrochloride
Featured
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SSD114 is a novel GABAB positive allosteric modulator. |
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| DC8896 |
Tiagabine hydrochloride
Featured
|
Tiagabine(NO328) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor. |
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| DC11319 |
TPMPA
Featured
|
TPMPA is a GABAA-ρ1 (ρ1 GABAC) receptor antagonist that is 8-fold selective for GABAA-ρ1 over GABAA-ρ2 (ρ2 GABAC) receptors expressed in X. |
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| DC9958 |
U 93631
Featured
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U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors. |
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| DC9560 |
Vigabatrin (Hydrochloride) |
Vigabatrin Hcl(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase.
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| DC9541 |
Vigabatrin
Featured
|
Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase.
IC50 value:
Target: GABA transaminase
Clinical studies have sh |
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| DC7642 |
Α5ia (α5IA) |
α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs. |
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| DC11117 |
KRM-II-81 |
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| DC28110 |
FG 7142
Featured
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the |
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| DC28164 |
Ro15-4513
Featured
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect. |
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| DC28546 |
Clomethiazole |
Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus. |
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| DC28579 |
(E)-GABAB receptor antagonist 1 |
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. |
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| DC40080 |
(2S)-6-Prenylnaringenin |
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface. |
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| DC40109 |
Broflanilide |
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM. |
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| DC40184 |
Etiocholanolone |
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form. |
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| DC40224 |
3-Methyl-GABA |
3-Methyl-GABA is an activator of GABA aminotransferase with anticonvulsant activity. |
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| DC40241 |
Flufiprole |
Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests. |
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| DC41026 |
COR659 |
COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats. |
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| DC41239 |
Tracazolate hydrochloride |
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity. |
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| DC42329 |
SJM-3 |
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at theα+/γ- subunit interface. |
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| DC42330 |
L-DAB HBR |
L-DAB HBR (L-DABA, L-2,4-Diaminobutyric acid) is an of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity. |
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| DC43984 |
2'MeO6MF |
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprot |
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| DC44564 |
Methionine |
Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity. |
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| DC44565 |
Etomidate hydrochloride |
Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity. |
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| DC44910 |
GABAA receptor agent 2 TFA |
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3). |
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| DC44911 |
Lesogaberan napadisylate |
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively. |
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| DC45866 |
Phaclofen |
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact. |
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| DC45881 |
CGP55845 hydrochloride |
CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research. |
|
| DC46019 |
Fengabine |
Fengabine is a GABAergic antidepressant drug. Fengabine can be used for the research of depression. |
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