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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

GABA transporters

" in MedChemExpress (MCE) Product Catalog:

18

Inhibitors & Agonists

3

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    CI-966 hydrochloride
  • HY-100809
    Guvacine hydrochloride

    		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).
    Guvacine hydrochloride
  • 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 .
    Arecaidine
  • 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 .
    Arecaidine hydrochloride
  • 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) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
    NNC 05-2090 hydrochloride
  • 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 .
    BPDBA
  • 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) .
    E2730
  • 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 .
    CI-966
  • 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 .
    3-Hydroxyphenazepam
  • 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 .
    Arecaidine hydrobromide
  • HY-103506
    NNC-711

    NO-711 hydrochloride

    		 GABA Receptor Neurological Disease
    NNC-711 is a potent and selective inhibitor of GAT-1 ( GABA transporter 1) with an IC50 of 40 nM for hGAT-1. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
    NNC-711
  • HY-100228A
    SKF89976A hydrochloride

    d,l-SKF89976A hydrochloride

    		 GABA Receptor Neurological Disease
    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.
    SKF89976A hydrochloride
  • HY-100228
    SKF 89976A

    		GABA Receptor Neurological Disease
    SKF89976A 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.
    SKF 89976A
  • 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 .
    BuChE-IN-9
  • 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 Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
    NNC 05-2090
  • 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 .
    LU-32-176B
  • HY-135482
    GABAA receptor agent 2 TFA

    		GABA Receptor Neurological Disease
    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) .
    GABAA receptor agent 2 TFA
  • HY-118931
    EF-1502

    		Others 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 .
    EF-1502

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