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Inhibitors & Modulators

Inhibitors and modulators are available for a wide range of transporter targets.

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Transporter Categories

ATP-binding Cassette Family

ATPases (F-type and V-type)

ATPases (P-type)

Major Facilitator Superfamily (MFS)

SLC Superfamily of Solute Carriers


ATP-binding Cassette Family

Gliclazide (SUR1 antagonist)


ATPases (F-type and V-type)

Abamectin (GABA antagonist, F0F1-ATPase and adenine nucleotide translocator inhibitor)

Citreoviridin A (F1F0 ATP synthase inhibitor)

Enterostatin (F1-ATPase inhibitor)

Nerolidol, synthetic (AChE inhibitor, F0F1-ATP synthase modulator)

Oligomycin A (F1F0 ATP synthase inhibitor)

Oligomycin B (F1F0 ATP synthase inhibitor)

Tentoxin (CF1 ATPase inhibitor)

ATPases (P-type)

2,5-Di-tert-butyl-4-hydroxyanisole (potential Ca2+ ATPase inhibitor)

Bisacodyl (Na+/K+ ATPase inhibitor)

Canrenone (Na+/K+ ATPase partial agonist, aldosterone and AR antagonist)

Cetrimide (H+ ATP synthase inhibitor)

Chelerythrine Chloride (PKC and Na+/K+ ATPase inhibitor)

Clotrimazole (14-α demethylase, H+/K+ ATPase, Na+/K+ ATPase inhibitor)

Cyclopiazonic Acid (SERCA inhibitor)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Esomeprazole Magnesium Trihydrate (H+/K+ ATPase inhibitor)

Esomeprazole Potassium (H+/K+ ATPase and MAO-A/B inhibitor)

Gastrin I (CCK2 agonist, indirect H+/K+ ATPase activator)

Isoflurane (Ca2+ ATPase and ATP-sensitive K+ channel activator, GABA-A and GlyR potentiator, NMDA antagonist, L-type Ca2+, delayed rectifier K+, A-type K+ channel blocker)

Lansoprazole (H+/K+ ATPase inhibitor)

Lopinavir (HIV protease inhibitor, SERCA inhibitor)

Oligomycin (oxidative phosphorylation inhibitor, potential Na+/K+ ATPase inhibitor)

Omeprazole (H+/K+ ATPase inhibitor)

Pantoprazole (H+/K+ ATPase and ROCK-2 inhibitor)

Pantoprazole Sodium Sesquihydrate (H+/K+ ATPase and ROCK-2 inhibitor)

Paxilline (BK K+ channel inhibitor, SERCA inhibitor)

Perillyl Alcohol (farnesyl transferase, geranylgeranyl transferase, telomerase, Na+/K+ ATPase inhibitor)

Protodioscin (Na+/K+ ATPase and Ca2+/Mg2+ ATPase activator)

Rabeprazole Sodium (H+/K+ ATPase and Scpc phosphatase inhibitor)

Tenatoprazole (H+/K+ ATPase inhibitor)

Thapsigargin (SERCA inhibitor)

Urodilatin CCC (Na+/K+ ATPase inhibitor)

Vindoline (Kv2.1 K+ channel blocker and H+/K+ ATPase inhibitor)

Major Facilitator Superfamily (MFS)

Levetiracetam (SV2A synaptic vesicle inhibitor)

SLC Superfamily of Solute Carriers

Amantadine Hydrochloride (Viral M2 proton channel blocker, MAO-A, NET, NMDA, α7 nAChR antagonist)

Amantadine Sulfate (Viral M2 proton channel blocker, MAO-A, NET, NMDA, α7 nAChR antagonist)

Amitriptyline Hydrochloride (FIASMA, σ1, RyR2, TrkA/B agonist, 5-HT2/6/7, M1-5 mAChR, histamine H1/4, α1-adr. antagonist, SERT, NET inhibitor, Kv1.1/7.2/7.3 K+, L-type Ca2+ channel blocker)

Amoxapine (5-HT2/3/6/7, D2/3/4, histamine H1, α1-adrenergic antagonist, SERT and NET inhibitor, hERG K+ channel blocker)

Aripiprazole (D2 and 5-HT1A partial agonist, 5-HT2C/6/7 antagonist, SERT inhibitor)

Atomoxetine Hydrochloride (NET and SERT inhibitor, NMDA antagonist)

Benztropine Mesylate (DAT inhibitor)

Brompheniramine Maleate (histamine H1 and mAChR antagonist, potential SERT and MAO-B inhibitor)

Bumetanide (NKCC symporter and KCC2 co-transporter inhibitor, potential GABA-A antagonist)

Chlorpheniramine Maleate (histamine H1 antagonist, SERT and NET inhibitor)

Citalopram Hydrobromide (SERT inhibitor)

Clomipramine Hydrochloride (FIASMA, mAChR, 5-HT2/3/6/7, α1/2-adrenergic antagonist, SERT and NET inhibitor, hERG K+ and L-type Ca2+ channel blocker)

Dapoxetine Hydrochloride (SERT inhibitor, potential voltage-gated K+ channel blocker)

Desvenlafaxine Succinate (SERT and NET inhibitor)

Dextromethorphan Hydrobromide Hydrate (σ1/2and μ/κ/δ-OR agonist, α3β4/α4β2/α7 nAChR, SERT, NET, NMDA antagonist)

Dihydrokainic Acid (NMDA agonist, GLT-1 inhibitor)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Duloxetine Hydrochloride (SERT and NET inhibitor, Nav1.7 Na+ channel blocker)

Escitalopram Oxalate (SERT inhibitor)

Fluoxetine Hydrochloride (FIASMA, SERT inhibitor, 5-HT and σ1 antagonist)

Fluvoxamine Maleate (FIASMA, 5-HT3 and σ1 agonist, SERT inhibitor)

Furosemide (NKCC symporter inhibitor, CFTR Cl- channel blocker, GABA-A antagonist)

Hydrochlorothiazide (NCCT inhibitor, carbonic anhydrase I inhibitor)

Indinavir Sulfate (HIV protease, GLUT4, calpain inhibitor)

Luteolin (DAT and NET potentiator, HSP90, IGF-1R, PDE inhibitor, potential α2-adrenergic antagonist)

Maprotiline Hydrochloride (FIASMA, histamine H1, 5-HT2, mAChR, α1-adrenergic antagonist, L-type Ca2+ channel blocker, NET inhibitor)

Nefazodone Hydrochloride (5-HT2 antagonist, SERT and NET inhibitor, hERG K+ channel blocker)

Paroxetine Hydrochloride Hemihydrate (FIASMA, SERT and NET inhibitor, mAChR antagonist)

Riluzole (TRPC5 agonist, PTR1 inhibitor, voltage-gated Na+ channel blocker, GLT-1 modulator)

Sertraline Hydrochloride (FIASMA, SERT and DAT inhibitor, α1-adrenergic antagonist, potential σ1 antagonist)

D-Tetrahydropalmatine (D1 antagonist, organic cation transporter 1 inhibitor)

Thioridazine Hydrochloride (FIASMA, D1-5, histamine H1/2, M1-5 mAChR, 5-HT1/2/5/6/7, α1/2-adrenergic antagonist, NET inhibitor, hERG K+ channel inhibitor)

Torsemide (NKCC symporter and HSP90 inhibitor)

Trazodone Hydrochloride (5-HT1A partial agonist, 5-HT2, histamine, α1/2-adrenergic antagonist, SERT inhibitor, voltage-gated K+ channel blocker)

Triacsin C (Acyl-CoA synthetase inhibitor)

Venlafaxine Hydrochloride (SERT, NET, MAO inhibitor)

Vilazodone (5-HT1A partial agonist, SERT inhibitor)

Vortioxetine (5-HT1A agonist, 5-HT1B partial agonist, 5-HT3A/7 antagonist, SERT inhibitor, potential β1-adrenergic agonist)