gaba uptake

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.

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

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, S(+)- is an inhibitor of GABA uptake.

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

NNC052090 is a GABA uptake inhibitor that displays moderate selectivity for BGT-1 transporters with Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively. NNC052090 also displays affinity at α1- and D2-receptors with IC50

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

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.

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.

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.

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

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

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

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, an alkaloid derived from the Areca catechu nut, serves as a potent inhibitor of GABA (GABA uptakp) uptake. It effectively inhibits rat GABA transporter isoforms GAT-1, GAT-2, and GAT-3, with respective IC50 values of 39 μM, 58 μM, and 378 μM [1].

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 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 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.