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Pathways Recommended:	Membrane Transporter/Ion Channel

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GABA transporters

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (30) 5-HT Receptor (1) Aminotransferases (Transaminases) (1) Beta-secretase (1) Cholinesterase (ChE) (1) Drug Metabolite (1) Isotope-Labeled Compounds (1) Reference Standards (5)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Neurological Disease (30)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Nucleoside Transporters GlyT GABA Receptor ATP-binding cassette (ABC) transporters ASCT

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-B0696

Tiagabine NO050328; NO328; TGB	GABA Receptor	Neurological Disease
Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-103504

(S)-SNAP5114 1 Publications Verification	GABA Receptor	Neurological Disease
(S)-SNAP5114 is a non-covalent murine *GABA* transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC₅₀=5.71, pK_i=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases .

HY-100228A

SKF89976A hydrochloride d,l-SKF89976A hydrochloride	GABA Receptor	Neurological Disease
SKF89976A hydrochloride is a selective **GABA transporter (GAT-1) inhibitor with IC₅₀**s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-100809

Guvacine hydrochloride 1 Publications Verification	GABA Receptor	Neurological Disease
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of **GABA transporter*, and dispalys modest selectivity for cloned GABA* transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

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-118301

ADX71441	GABA Receptor 5-HT Receptor	Neurological Disease
ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABA_B receptor. ADX71441 potentiates the activity of endogenous GABA at GABA_B receptor, with an EC₅₀ of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT_2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .

HY-W067716

Spinacine (S)-Spinacine	GABA Receptor	Neurological Disease
Spinacine ((S)-Spinacine) is a GABA uptake inhibitor. Spinacine enhances synaptic GABA effects via inhibition of gamma-aminobutyric acid uptake in cerebral cortex slices. Spinacine inhibits reflex responses of ventral roots in isolated spinal cord. Spinacine inhibits motor activity and reduces approaches to water dispensers in conflict situations. Spinacine raises pain sensitivity threshold via subarachnoidal injection .

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-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-103506

NNC-711 NO-711 hydrochloride	GABA Receptor	Neurological Disease
NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC₅₀ values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .

HY-N2368B

Arecaidine hydrobromide 1 Publications Verification	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-119591

BPDBA	GABA Receptor	Neurological Disease
BPDBA is a selective and noncompetitive betaine/GABA transporter (BGT-1) inhibitor with IC₅₀s of 20 μM and 35 μM against human BGT-1 and mouse GAT2, respectively .

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-118931

EF-1502	GABA Receptor	Neurological Disease
EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitory activity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy .

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-N2368AR

Arecaidine hydrochloride (Standard)	Reference Standards 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-100228

SKF 89976A	GABA Receptor	Neurological Disease
SKF89976A is a selective **GABA transporter (GAT-1) inhibitor with IC₅₀**s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-155305

BuChE-IN-9	Cholinesterase (ChE) Beta-secretase GABA Receptor	Neurological Disease
BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC₅₀ of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties .

HY-W740245

Arecaidine-d5 hydrobromide	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Arecaidine-d₅ hydrobromide is the deuterium labeled Arecaidine hydrobromide (HY-N2368B). 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-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 .

HY-118207

LU-32-176B	GABA Receptor	Cancer
LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively .

HY-135482

GABAA receptor agent 2 TFA	GABA Receptor	Neurological Disease
GABAA receptor agent 2 TFA is a potent and high-affinity GABA_A receptor antagonist with an IC₅₀ of 24 nM (human α1β2γ2 GABA_A-expressing tsA201 cells) and a K_i of 28 nM (rat GABA_A receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .

HY-181961

SR-THAP	GABA Receptor	Cardiovascular Disease Neurological Disease
SR-THAP is a γ-aminobutyric acid transporter 3 (GAT3) inhibitor with an IC₅₀ of 4.9 μM, and exhibits 42-fold and 23-fold selectivity over GAT1 and GlyT1, respectively. SR-THAP inhibits GABA uptake in mammalian cells. SR-THAP is applicable to the research of epilepsy, Alzheimer's disease and ischemic stroke .

HY-103534R

CI-966 hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. 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-182944

GATT-44	GABA Receptor	Neurological Disease
GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC₅₀ of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated ¹⁸F-radiofluorination. The radiolabeled GATT-44 ([ ¹⁸F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases .

HY-181135

Bicyclo-GABA	GABA Receptor	Neurological Disease
Bicyclo-GABA is a selective *betaine/GABA* transporter 1 (BGT1)** competitive, non-transported inhibitor with an IC₅₀ of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α₁β₂γ₂ GABA_A receptors with an EC₅₀ of 5.1 μM. Bicyclo-GABA displays 129 times higher activity for BGT1 than GAT3. Bicyclo-GABA serves as a valuable tool compound for deciphering its elusive pharmacological role in the brain and periphery .

HY-W1025152

CPP-115 hydrochloride	Aminotransferases (Transaminases) GABA Receptor	Neurological Disease
CPP-115 hydrochloride is an orally active, selective *GABA-AT* inhibitor with a K_i value of 9.7 μM. CPP-115 hydrochloride blocks *GABA* degradation and increases GABA levels in the brain. CPP-115 hydrochloride does not bind to GABA transporters, does not displace GABA from GABA_A/GABA_B receptors, and does not act as an agonist/antagonist of GABA_C receptors. CPP-115 hydrochloride reduces cocaine-induced dopamine release, blocks cocaine-induced conditioned place preference, and suppresses seizure activity in a rat model of infantile spasms. CPP-115 hydrochloride can be used in research related to infantile spasms and epilepsy .

HY-103509R

NNC 05-2090 hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
NNC 05-2090 hydrochloride (Standard) is the analytical standard of NNC 05-2090 hydrochloride (HY-103509). This product is intended for research and analytical applications. NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC₅₀< /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-100228AR

SKF89976A hydrochloride (Standard) d,l-SKF89976A hydrochloride (Standard)	GABA Receptor Reference Standards	Neurological Disease
SKF89976A (hydrochloride) (Standard) is the analytical standard of SKF89976A (hydrochloride) (HY-100228A). This product is intended for research and analytical applications. SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-103506R

NNC-711 (Standard) NO-711 hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
NNC-711 (Standard) is the analytical standard of NNC-711 (HY-103506). This product is intended for research and analytical applications. NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC₅₀ values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .

Cat. No.	상품명	Category	Target	Chemical Structure

HY-100809

Guvacine hydrochloride 1 Publications Verification	Alkaloids Classification of Application Fields Neurological Disease Areca catechu L. Pyridine Alkaloids Plants Palmae Disease Research Fields Source Classification	GABA Receptor
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of **GABA transporter*, and dispalys modest selectivity for cloned GABA* transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

HY-N2368A

Arecaidine hydrochloride 1 Publications Verification	Alkaloids Areca catechu L. Pyridine Alkaloids Plants Palmae Source Classification	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-W067716

Spinacine (S)-Spinacine	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	GABA Receptor
Spinacine ((S)-Spinacine) is a GABA uptake inhibitor. Spinacine enhances synaptic GABA effects via inhibition of gamma-aminobutyric acid uptake in cerebral cortex slices. Spinacine inhibits reflex responses of ventral roots in isolated spinal cord. Spinacine inhibits motor activity and reduces approaches to water dispensers in conflict situations. Spinacine raises pain sensitivity threshold via subarachnoidal injection .

HY-N2368AR

Arecaidine hydrochloride (Standard)	Structural Classification Alkaloids Areca catechu L. Pyridine Alkaloids Plants Palmae Source Classification	Reference Standards 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 .

Cat. No.	상품명	Chemical Structure

HY-W740245

Arecaidine-d5 hydrobromide
Arecaidine-d₅ hydrobromide is the deuterium labeled Arecaidine hydrobromide (HY-N2368B). 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 .

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GABA transporters

Inhibitors & Agonists

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Isotope-Labeled Compounds

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