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Results for "

GABA uptake

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (24) Chloride Channel (2) Drug Metabolite (1) Isotope-Labeled Compounds (1) Parasite (2) Sodium Channel (4)
By Research Areas:	Cancer (3) Infection (2) Neurological Disease (22)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: GABA Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-69359

Nipecotic acid (±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine	GABA Receptor	Neurological Disease
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABA_A-like chloride channels, with an EC₅₀ of approximately 300?μM .

HY-B0696A

Tiagabine hydrochloride NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride	GABA Receptor	Neurological Disease
Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC₅₀s of 67, 446 and 182 nM for [ ³H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .

HY-100800

TACA trans-4-Aminocrotonic acid	GABA Receptor	Neurological Disease
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABA_A and GABA_C receptors (K_D= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .

HY-16974

Afoxolaner	GABA Receptor Chloride Channel Parasite	Infection
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .

HY-129464

NO-711ME	GABA Receptor	Neurological Disease
NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor .

HY-N9407

Guvacine ethyl ester	GABA Receptor	Others
Guvacine ethyl ester (3.1b) is an alkaloid that can be found in betel nut. Guvacine ethyl ester can be used in the synthesis of GABA uptake inhibitor .

HY-124030

3-Hydroxyphenazepam	Drug Metabolite	Neurological Disease
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ ³H]GABA uptake .

HY-W103105

R 29676	GABA Receptor	Neurological Disease
R 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake) .

HY-B0696B

Tiagabine hydrochloride hydrate NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate	GABA Receptor	Neurological Disease
Tiagabine hydrochloride hydrate is a potent and selective **GABA uptake inhibitor, used as an anticonvulsant agent, with IC₅₀*s of 67, 446 and 182 nM for [ ³H]GABA* uptake in Synaptosomes, Neurons and Glia, respectively .

HY-B0696

Tiagabine NO050328; NO328; TGB	GABA Receptor	Neurological Disease
Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC₅₀s of 67, 446 and 182 nM for [ ³H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .

HY-B0696AS

Tiagabine-d4 hydrochloride NO050328-dd₄ hydrochloride; NO328-d₄ hydrochloride; TGB-d₄ hydrochloride	GABA Receptor Isotope-Labeled Compounds	Neurological Disease
Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC₅₀s of 67, 446 and 182 nM for [ ³H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .

HY-B0211

Riluzole Maximum Cited Publications 9 Publications Verification PK 26124	Sodium Channel GABA Receptor	Neurological Disease Cancer
Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na ⁺ channel blocker which can also inhibit *GABA* uptake with an IC₅₀ of 43 μM.

HY-B0211A

Riluzole hydrochloride Maximum Cited Publications 9 Publications Verification PK 26124 hydrochloride	Sodium Channel GABA Receptor	Neurological Disease Cancer
Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na ⁺ channel blocker which can also inhibit *GABA* uptake with an IC₅₀ of 43 μM.

HY-N2368

Arecaidine 1 Publications Verification	GABA Receptor	Neurological Disease
Arecaidine, a pyridine alkaloid, is a potent **GABA uptake** inhibitor. Arecaidine is a substrate of H ⁺-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .

HY-N2368A

Arecaidine hydrochloride 1 Publications Verification	GABA Receptor	Neurological Disease
Arecaidine hydrochloride, a pyridine alkaloid, is a potent **GABA uptake** inhibitor. Arecaidine hydrochloride is a substrate of H ⁺-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .

HY-N2368B

Arecaidine hydrobromide	GABA Receptor	Neurological Disease
Arecaidine hydrobromide, a pyridine alkaloid, is a potent **GABA uptake** inhibitor. Arecaidine hydrobromide is a substrate of H ⁺-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .

HY-103534

CI-966 hydrochloride	GABA Receptor	Neurological Disease
CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities .

HY-123240

CI-966	GABA Receptor	Neurological Disease
CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities .

HY-103509

NNC 05-2090 hydrochloride	GABA Receptor	Neurological Disease
NNC 05-2090 hydrochloride is a *GABA* uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC_{50< /sub>}: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a K_i value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .

HY-16974R

Afoxolaner (Standard)	GABA Receptor Chloride Channel Parasite	Infection
Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .

HY-114040

NO-711 NNC-711 free acid	GABA Receptor	Neurological Disease
NO-711 (NNC-711) free acid is a novel potent and selective inhibitor of γ-aminobutyric acid uptake. NO-711 inhibits synaptosomal (IC₅₀ = 47 nM), neuronal (IC₅₀ = 1238 nM) and glial (IC₅₀ = 636 nM) GABA uptake in vitro .

HY-B0211R

Riluzole (Standard) PK 26124 (Standard)	Sodium Channel GABA Receptor	Neurological Disease Cancer
Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na ⁺ channel blocker which can also inhibit *GABA* uptake with an IC₅₀ of 43 μM.

HY-155238

E2730	GABA Receptor	Neurological Disease
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .

HY-B0211S

Riluzole-13C,15N2 PK 26124-¹³C,¹⁵N₂	GABA Receptor Sodium Channel	Neurological Disease
Riluzole- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].

HY-120146

NNC 05-2090	GABA Receptor	Neurological Disease
NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC₅₀ sub>: 10.6 μM). NNC 05-2090 also inhibits mGAT2 with a K_i value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2368

Arecaidine 1 Publications Verification	Alkaloids Areca catechu L. Source classification Pyridine Alkaloids Plants Palmae	GABA Receptor
Arecaidine, a pyridine alkaloid, is a potent **GABA uptake** inhibitor. Arecaidine is a substrate of H ⁺-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .

HY-N2368A

Arecaidine hydrochloride 1 Publications Verification	Alkaloids Structural Classification Areca catechu L. Source classification Pyridine Alkaloids Palmae Plants	GABA Receptor
Arecaidine hydrochloride, a pyridine alkaloid, is a potent **GABA uptake** inhibitor. Arecaidine hydrochloride is a substrate of H ⁺-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .

HY-N9407

Guvacine ethyl ester	Alkaloids Structural Classification Classification of Application Fields Areca catechu L. Source classification Other Diseases Pyridine Alkaloids Plants Palmae Disease Research Fields	GABA Receptor
Guvacine ethyl ester (3.1b) is an alkaloid that can be found in betel nut. Guvacine ethyl ester can be used in the synthesis of GABA uptake inhibitor .

Cat. No.	Product Name	Chemical Structure

HY-B0696AS

Tiagabine-d4 hydrochloride
Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC₅₀s of 67, 446 and 182 nM for [ ³H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .

HY-B0211S

Riluzole-13C,15N2
Riluzole- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].

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GABA uptake

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
Products