gaba uptake

NO-711ME (N-O711 Methyl ester) is a prodrug of NO-711. It also is a potent and selective GABA uptake inhibitor.

Riluzole hydrochloride (PK 26124 hydrochloride) is an anticonvulsant compound belonging to the family of sodium channel blockers that inhibits GABA uptake.Riluzole hydrochloride is a sodium-glutamate antagonist with anticancer and neuroprotective activity and can be used to study amyotrophic lateral sclerosis and neurological disorders.

Tiagabine hydrochloride (NO050328 hydrochloride) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)

Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

(+)-Nipecotic acid ((+)-β-Homoproline) is a specific inhibitor of GABA transport and uptake, capable of activating GABAA receptors and elevating endogenous GABA concentrations, suitable for psychiatric disorder research.

D-DABA is the enantiomer of L-DABA. It acts as a weak inhibitor of GABA-T, but its effectiveness in inhibiting GABA uptake is just one-twentieth that of L-DABA.

(±)-Nipecotic acid is a GABA uptake inhibitor.

NNC 05-2090 is a GABA uptake inhibitor that exhibits moderate selectivity for BGT-1 transporters over other GABA transporter subtypes, while also displaying measurable affinity toward α1-adrenergic and D2-dopaminergic receptors, making NNC 05-2090 a multifunctional neuropharmacological tool for investigating inhibitory neurotransmission and transporter-receptor cross-regulation.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

Arecaidine hydrochloride may have carcinogenesis.

Tiagabine hydrochloride hydrate is a potent and selective inhibitor of GABA uptake, inhibiting [3H] GABA uptake in synaptosomes, neurons, and glia with IC50 values of 67, 446, and 182 nM, respectively. This hydrate can be used as an anticonvulsant.

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.

Gaboxadol hydrobromide is a GABA agonist. It is an inhibitor of GABA uptake systems. Gaboxadol can also be a non-opioid analgesic and a novel type of hypnotic.

(±)-Homoproline Hydrochloride functions as a γ-aminobutyric acid (GABA) uptake inhibitor structurally derived from proline.

(+/-)-Homoproline is a GABA-uptake inhibitor derived from proline.

Arecaidine hydrobromide is the salt form of Arecaidine, a pyridine alkaloid with potent GABA uptake inhibitory properties that acts as a substrate for H+-coupled amino acid transporter protein 1 (PAT1, SLC36A1) to competitively inhibit the uptake of L-proline.

Guvacine hydrobromide is an alkaloid discovered in Areca catechu and a GABA uptake inhibitor with IC50 values of 39 μM/58 μM/378 μM for rat GAT-1/GAT-2/GAT-3.

Guvacine ethyl ester (Arecoline) is an alkaloid found in betel nut that is used in the synthesis of GABA uptake inhibitors.

Zonisamide-D4 is a deuterated compound of Zonisamide. Zonisamide (T0267) has a CAS number of 68291-97-4. Zonisamide, a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide (T0267) may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Afoxolaner (Standard) is the standard substance of Afoxolaner, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

Bumetanide (Standard) is the standard substance of Bumetanide, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.