Ion Channel Modulators

5-HT3 Receptors

Acid-sensing Channels

Calcium Channels

Chloride Channels

CNG Channels

GABA Receptors

Gap Junction Channels

Glycine Receptors

Ionotropic Glutamate Receptors

Nicotinic Acetylcholine Receptors

P2X Receptors

Potassium Channels

Ryanodine Receptors

Sodium Channels

Transient Receptor Potential Channels

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)

Dolasetron (5-HT3 antagonist)

Dolasetron Mesylate Hydrate (5-HT3 antagonist)

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

8-Gingerol (5-HT3 antagonist)

10-Gingerol (5-HT3 antagonist)

Granisetron Hydrochloride (5-HT3 antagonist)

Memantine Hydrochloride (D2 agonist, NMDA, 5-HT3, α7 nAChR antagonist)

5-Methoxyindole (potential PPARγ and 5-HT3 agonist)

Ondansetron Hydrochloride Dihydrate (5-HT3 antagonist)

Ramosetron (5-HT3 antagonist)

Shogaol (PPARγ agonist, 5-HT3 antagonist)

Tropisetron Hydrochloride (α7 nAChR partial agonist, 5-HT3 antagonist)

Amiloride Hydrochloride Dihydrate (ENaC and acid-sensing ion channel blocker, Na+/H+ antiporter inhibitor)

Oxytocin (OXTR agonist, acid-sensing ion channel blocker)

RF-NH2 (potential GPR147 agonist, potential acid-sensing ion channel activator)

Sinomenine Hydrochloride (acid-sensing ion channel and L-type Ca2+ channel blocker)

Allicin (inwardly rectifying K+ channel activator, L-type Ca2+ channel blocker)

Allicin, aqueous (Kir K+ channel activator, L-type Ca2+ channel blocker)

Amiodarone Hydrochloride (Voltage-gated Na+, Ca2+, K+ channel blocker, α/β-adrenergic antagonist, FIASMA)

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)

Amlodipine (FIASMA; L-type Ca2+ channel blocker)

Amlodipine Besylate (FIASMA; L-type Ca2+ channel blocker)

Catharanthine base (voltage-gated Ca2+ channel blocker)

Catharanthine Sulfate (voltage-gated Ca2+ channel blocker)

Catharanthine Tartrate (voltage-gated Ca2+ channel blocker)

Cilnidipine (L-type and N-type Ca2+ channel blocker)

Cinnarizine (FIASMA, L-type Ca2+ channel blocker, D2 antagonist)

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)

Cyproconazole (14-α demethylase inhibitor, voltage-gated Ca2+ channel blocker, potential aromatase inhibitor)

Dantrolene Sodium Heptahydrate (RyR antagonist, L-type Ca2+ channel blocker)

Deoxyandrographolide (cNOS and adenylyl cyclase activator, PAF inhibitor, potential voltage-gated Ca2+ channel blocker)

Dihydromethysticin (Voltage-gated Na+ and L-type Ca2+ channel blocker)

Diltiazem Hydrochloride (L-type Ca2+ channel blocker, potential CNG channel blocker)

Dimebon Dihydrochloride (AMPK activator, L-type Ca2+ channel and NMDA, histamine H1/2, α-adrenergic, 5-HT2C/5A/6 receptor antagonist)

Felodipine (L-type Ca2+ channel blocker)

Gabapentin (GABA potentiator, adenosine A1 agonist, voltage-gated α2δ Ca2+ channel blocker, NMDA modulator)

Glucagon (19-29), human (potential Ca2+ channel blocker)

Hesperetin (L-type Ca2+ channel blocker)

Hypericin (dopamine β-hydroxylase and proteasome inhibitor, N-type and P/Q-type Ca2+ channel blocker)

Kawain (Voltage-gated Na+ and L-type Ca2+ channel blocker)

Lamotrigine (R-type Ca2+ and voltage-gated Na+ channel blocker)

Lomerizine Dihydrochloride (L-type and T-type Ca2+ and TRP antagonist)

Manidipine Dihydrochloride (L-type and N-type Ca2+ channel blocker)

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

Nefiracetam (NMDA and mGluR5 agonist, N-type and L-type Ca2+ channel activator, α4β2 nAChR potentiator)

Nicardipine (L-type Ca2+ channel blocker)

Nifedipine (L-type Ca2+ channel blocker)

Niflumic Acid (NMDA inverse agonist, T-type Ca2+ and Cl- channel blocker, GABA-A antagonist, COX-1/2 inhibitor)

Nimodipine (L-type Ca2+ channel blocker)

Paeoniflorin (L-type Ca2+ channel blocker)

Paeonol (MAO-A/B inhibitor, voltage-gated and receptor-gated Ca2+ channel blocker)

Panaxadiol (voltage-gated Ca2+ channel blocker)

Panaxatriol (voltage-gated Ca2+ channel blocker)

Penicillic Acid (BK K+, voltage-gated cardiac Na+, K+, Ca2+ channel inhibitor)

Praziquantel (potential adenosine antagonist, potential voltage-gated Ca2+ channel blocker)

Protopine (voltage- and receptor-gated Ca2+ channel blocker)

Rhyncholphylline (hERG K+ and L-type Ca2+ channel channel blocker, NMDA antagonist)

Roscovitine (CDK inhibitor, L-type Ca2+ channel blocker)

Simvastatin (HMG-CoA reductase inhibitor, potential ATP-sensitive K+ channel activator, L-type Ca2+ channel blocker)

Sinomenine Hydrochloride (acid-sensing ion channel and L-type Ca2+ channel blocker)

Snake venom - Crotalus durissus terrificus (binds N-type and P/Q-type Ca2+ channels, L-type Ca2+ channel potentiator, NMJ blocker)

Somatostatin-14 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-25 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-12) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-14) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr1]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr11]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Tebuconazole (14-α demethylase inhibitor, voltage-gated Ca2+ channel blocker, potential aromatase inhibitor)

S,S-(+)-Tetrandrine (voltage-gated Ca2+ channel blocker)

D,L-Tetrahydropalmatine (D1/2 antagonist, potential L-type Ca2+ and K+ channel blocker)

Trimebutine Base (BK K+ channel and L-type Ca2+ channel blocker)

Trimebutine Maleate (L-type Ca2+ channel blocker, BK K+ channel modulator, potential opioid agonist)

Valproic Acid Sodium (T-type Ca2+ and voltage-gated Na+ channel blocker, GABA transaminase and HDAC inhibitor)

Verapamil Hydrochloride (L-type Ca2+ channel blocker)

Zonisamide (carbonic anhydrase inhibitor, voltage-gated Na+ and T-type Ca2+ channel blocker)

Aloe Emodin (CTFR Cl- channel activator)

Cromolyn Sodium (potential TRP antagonist, potential Cl- channel blocker)

Emodin (CTFR Cl- channel activator)

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

Ivermectin (glu-gated Cl- channel activator, GlyR and GABA-A agonist)

Niflumic Acid (NMDA inverse agonist, T-type Ca2+ and Cl- channel blocker, GABA-A antagonist, COX-1/2 inhibitor)

Triacetyl Aloe-emodin (Impurity A) (CFTR Cl- channel activator)

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)

Diltiazem Hydrochloride (L-type Ca2+ channel blocker, potential CNG channel blocker)

KT5720 (PKA and PDK1 inhibitor, HCN channel blocker, potential GSK3, MEK, MSK1, PKB inhibitor)

Loperamide Hydrochloride (FIASMA, μOR agonist, potential HCN channel blocker)

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

Apigenin (GABA-A positive modulator, potential microtubule depolymerization inducer)

Baclofen (GABA-B agonist)

(−)-Bilobalide (GABA-A antagonist)

(+)-Bicuculline (NMDA potentiator, GABA-A antagonist)

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

Dehydroepiandrosterone (ERβ, NMDA, σ1 agonist, ERα and AR partial agonist, GABA-A antagonist)

Delta Sleep Inducing Peptide (GABA potentiator, NMDA negative allosteric modulator)

Emamectin B1 Benzoate (GABA potentiator)

Eprinomectin (GABA potentiator)

Etomidate (GABA-A agonist)

Flumazenil (GABA-A antagonist)

Flumequine Sodium (bacterial DNA gyrase inhibitor, GABA-A antagonist)

Flupirtine Maleate (Kv7 K+ channel activator, NMDA antagonist, GABA-A negative modulator)

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

Gabapentin (GABA potentiator, adenosine A1 agonist, voltage-gated α2δ Ca2+ channel blocker, NMDA modulator)

Ginkgolide C (GABA-A, α-1 GlyR, PAF antagonist)

Ginsenoside Rg3 (γ2 GABA-A agonist, Kv7.1 K+ channel activator, α10 nAChR antagonist)

20S-Ginsenoside Rg3 (Kv7.1 K+ channel activator, γ2 GABA-A agonist, α10 nAChR antagonist)

Glabridin (GABA-A positive modulator)

Honokiol (GABA-A potentiator)

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)

Ivermectin (glu-gated Cl- channel activator, GlyR and GABA-A agonist)

Magnolol (GABA-A potentiator)

Mefenamic Acid (GABA-A potentiator, COX-1/2 inhibitor)

Nicotinamide (GABA modulator)

Niflumic Acid (NMDA inverse agonist, T-type Ca2+ and Cl- channel blocker, GABA-A antagonist, COX-1/2 inhibitor)

Penitrem A (GABA-A potentiator, BK K+ channel inhibitor)

Pregnenolone (TRPM3 agonist, NMDA potentiator, GABA-A negative allosteric modulator)

Protopanaxadiol (GABA-A antagonist)

Protopanaxatriol (GABA-A/C antagonist, slow-activating delayed rectifier K+ channel blocker)

Puerarin (5-HT2C and GABA-A antagonist)

Puerarin (GABA-A potentiator, 5-HT2C antagonist)

Rosmarinic Acid (GABA transaminase and Fyn kinase inhibitor)

Securinine (potential GABA-A antagonist)

Somatostatin-14 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-25 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-12) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-14) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr1]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr11]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Taurine (GABA-A and GlyR agonist)

Verruculogen (BK K+ channel blocker, GABA-A antagonist)

Yangonin (CB1 agonist, GABA-A potentiator)

γ-Amino Butyric Acid (GABA agonist)

Carbenoxolone (11β-HSD inhibitor, gap junction connexin channel blocker)

Carbenoxolone Disodium (connexin and 11β-hydroxysteroid dehydrogenase inhibitor)

Ginkgolide B (GlyR antagonist)

Ginkgolide C (GABA-A, α-1 GlyR, PAF antagonist)

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)

Ivermectin (glu-gated Cl- channel activator, GlyR and GABA-A agonist)

Taurine (GABA-A and GlyR agonist)

L-Alliin (NMDA NR2A/2B agonist)

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)

trans-Anethole (NMDA agonist)

Aniracetam (AMPA positive allosteric modulator, D2, 5-HT2A, nAChR agonist)

Atomoxetine Hydrochloride (NET and SERT inhibitor, NMDA antagonist)

(+)-Bicuculline (NMDA potentiator, GABA-A antagonist)

Chlortetracycline Hydrochloride (protein translation inhibitor, MMP and calpain inhibitor, NMDA antagonist)

D-Cycloserine (NMDA partial agonist, D-Ala-D-Ala ligase inhibitor)

Dehydroepiandrosterone (ERβ, NMDA, σ1 agonist, ERα and AR partial agonist, GABA-A antagonist)

Delta Sleep Inducing Peptide (GABA potentiator, NMDA negative allosteric modulator)

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)

Dimebon Dihydrochloride (AMPK activator, L-type Ca2+ channel and NMDA, histamine H1/2, α-adrenergic, 5-HT2C/5A/6 receptor antagonist)

Flupirtine Maleate (Kv7 K+ channel activator, NMDA antagonist, GABA-A negative modulator)

Flutriafol (demethylation inhibitor, NMDA agonist)

Gabapentin (GABA potentiator, adenosine A1 agonist, voltage-gated α2δ Ca2+ channel blocker, NMDA modulator)

(−)-Huperzine A (AChE inhibitor, NMDA antagonist)

Kainic Acid (AMPA and kainate agonist)

Memantine Hydrochloride (D2 agonist, NMDA, 5-HT3, α7 nAChR antagonist)

Nefiracetam (NMDA and mGluR5 agonist, N-type and L-type Ca2+ channel activator, α4β2 nAChR potentiator)

Niflumic Acid (NMDA inverse agonist, T-type Ca2+ and Cl- channel blocker, GABA-A antagonist, COX-1/2 inhibitor)

Nobiletin (potential AMPA positive modulator)

Pregnenolone (TRPM3 agonist, NMDA potentiator, GABA-A negative allosteric modulator)

Rhyncholphylline (hERG K+ and L-type Ca2+ channel channel blocker, NMDA antagonist)

Risperidone (5-HT7 and NMDA agonist, D-amino acid oxidase inhibitor, 5-HT2A and D2 antagonist)

Sulfasalazine (sepiapterin reductase inhibitor, NMDA antagonist)

L-Theanine (weak AMPA and NMDA agonist)

Trimetazidine (Long-chain 3-ketoacyl-CoA thiolase inhibitor, potential kainate and AMPA antagonist)

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)

Anabasine Hydrochloride (depolarizing NMJ blocker; nAChR antagonist, aromatase inhibitor, teratogen)

Aniracetam (AMPA positive allosteric modulator, D2, 5-HT2A, nAChR agonist)

Atracurium Besylate (AChR antagonist)

Bupropion Hydrochloride (α3β2, α3β4, α4β2 nAChR antagonist, indirect DA and NE reuptake inhibitor)

Cisatracurium Besylate (nAChR and M2 mAChR antagonist)

α-Conotoxin GI (nAChR inhibitor)

α-Conotoxin IMI (α7 nAChR inhibitor)

Cytisine (α3β4 nAChR agonist, α4β2 partial agonist)

13-Desmethyl Spirolide C (nAChR and mAChR antagonist)

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

Dimethyl Fumarate (nAChR agonist, indirect Nrf2 activator)

Galantamine Hydrobromide (AChE inhibitor, α7 nAChR agonist, mAChR agonist)

Ginsenoside Rg3 (γ2 GABA-A agonist, Kv7.1 K+ channel activator, α10 nAChR antagonist)

20S-Ginsenoside Rg3 (Kv7.1 K+ channel activator, γ2 GABA-A agonist, α10 nAChR antagonist)

Hexamethonium Bromide Hydrate (nAChR antagonist)

Levamisole Hydrochloride (alkaline phosphatase inhibitor, potential nAChR agonist)

Mecamylamine Hydrochloride (nAChR antagonist)

Memantine Hydrochloride (D2 agonist, NMDA, 5-HT3, α7 nAChR antagonist)

12-Methyl Gymnodimine (nAChR antagonist)

Mivacurium Chloride (nAChR antagonist)

Nefiracetam (NMDA and mGluR5 agonist, N-type and L-type Ca2+ channel activator, α4β2 nAChR potentiator)

Nordihydroguaiaretic Acid (5-lipoxygenase, AChR, BChE, mTORC1 inhibitor)

Oxcarbazepine (α4β2 nAChR desensitizer, delayed-rectifier voltage-gated K+ and voltage-gated Na+ channel blocker)

Pancuronium Bromide (nAChR antagonist)

Penicillin G procaine (penicillin binding protein inhibitor, potential nAChR antagonist)

Progesterone (PR agonist, mineralocorticoid, nAChR, σ1/2 antagonist)

Pyrantel Pamoate (nAChR inhibitor)

Rocuronium Bromide (nAChR and M2/3 mAChR antagonist)

Tropisetron Hydrochloride (α7 nAChR partial agonist, 5-HT3 antagonist)

Vecuronium Bromide (nAChR antagonist)

Neomycin Sulfate (protein translation inhibitor, cation channel/receptor (P2X, TRPV1) blocker)

Paromomycin Sulfate (protein translation inhibitor, cation (PX2X) channel blocker)

Spinorphin, cow (P2X3 and N-formylpeptide antagonist, ACE, enkephalinase, aminopeptidase IV, neutral endopeptidase, DPP3 inhibitor)

Allicin (inwardly rectifying K+ channel activator, L-type Ca2+ channel blocker)

Allicin, aqueous (Kir K+ channel activator, L-type Ca2+ channel blocker)

Amiodarone Hydrochloride (Voltage-gated Na+, Ca2+, K+ channel blocker, α/β-adrenergic antagonist, FIASMA)

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

Amsacrine (topoisomerase II inhibitor, hERG K+ channel blocker)

Apamin (SK2/3/4 K+ channel blocker)

Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

[Tyr4]-Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

Bupivacaine (BK/SK, Kv1, Kv3, TASK-2 K+ channel blocker, voltage-gated Na+ channel blocker)

Bupivacaine Hydrochloride Monohydrate (voltage-gated Na+, BK/SK, Kv1, Kv3, TASK-2 K+ channel inhibitor)

Carbamazepine (voltage-gated Na+ and ATP-sensitive K+ channel blocker)

Catch-Relaxing Peptide (BK/SK K+ channel modulator)

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)

Clozapine (M4 mAChR agonist, 5-HT1A partial agonist, M1/2/3/5 mAChR, D2 antagonist, Kv1.1 K+ channel blocker)

Cyclovirobuxine D (hERG K+ channel inhibitor)

Cytochalasin A (actin polymerization inhibitor, Kv1.5 K+ channel blocker.)

Diclofenac Sodium (COX-1/2 inhibitor, potential K+ channel modulator)

Dihydrocytochalasin B (actin polymerization inhibitor, Kv1.1-A-type K+ channel converter)

α,β-Dihydroresveratrol (potential voltage-gated K+ channel modulator)

Domperidone (D2/3 antagonist, hERG K+ channel blocker)

Doxapram Hydrochloride Hydrate (K+ channel blocker, catecholamine release stimulator)

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

Efaroxan Hydrochloride (α2-adrenergic and imidazoline-1 antagonist, ATP-sensitive K+ channel blocker)

Flufenamic Acid (TREK1 K+ potentiator, voltage-gated Na+ channel blocker, TRPC3 and TRPM2 antagonist, COX-1/2 inhibitor)

Fluphenazine Hydrochloride (FIASMA, D2 antagonist, hERG K+ channel blocker)

Flupirtine Maleate (Kv7 K+ channel activator, NMDA antagonist, GABA-A negative modulator)

FMRF Amide (delayed rectifier K+ channel modulator)

FMRF-like Peptide, snail (delayed rectifier K+ channel modulator)

Ginsenoside Rg3 (γ2 GABA-A agonist, Kv7.1 K+ channel activator, α10 nAChR antagonist)

20S-Ginsenoside Rg3 (Kv7.1 K+ channel activator, γ2 GABA-A agonist, α10 nAChR antagonist)

Glimepiride (ATP-sensitive K+ channel blocker)

Glipizide (ATP-sensitive K+ channel blocker)

18β-Glycyrrhetinic Acid (15-HPGDH inhibitor, hERG and KCNA3/Kv1.3 K+ channel blocker)

Iloperidone (D2 and 5-HT2A antagonist, potential hERG K+ channel blocker)

Imiquimod (TLR-7/8 agonist, KCNA1/Kv1.1 and KCNA2/Kv1.2 K+ channel partial agonist, TREK-1/K2P2 and TRAAK/K2P4 K+ channel blocker)

Indapamide (Kv7.1 and minK K+ channel blocker)

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)

Levosimendan (Ca2+ sensitizer; ATP-sensitive K+ channel activator, troponin C stabilizer, PDE inhibitor)

Mitiglinide Calcium (ATP-sensitive K+ channel blocker, potential RyR agonist)

Moguisteine (Potential ATP-sensitive K+ channel blocker, potential irritant receptor antagonist)

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

Nifekalant Hydrochloride (Voltage-gated K+ channel blocker)

Nocistatin (TRPC agonist, BK/SK K+ channel modulator)

Oxcarbazepine (α4β2 nAChR desensitizer, delayed-rectifier voltage-gated K+ and voltage-gated Na+ channel blocker)

Paxilline (BK K+ channel inhibitor, SERCA inhibitor)

Penicillic Acid (BK K+, voltage-gated cardiac Na+, K+, Ca2+ channel inhibitor)

Penitrem A (GABA-A potentiator, BK K+ channel inhibitor)

Phentolamine Hydrochloride (ATP-sensitive K+ channel activator, α-adrenergic antagonist)

Phentolamine Methanesulfonate (ATP-sensitive K+ channel activator, α-adrenergic antagonist)

Pipemidic Acid (bacterial DNA gyrase inhibitor and ATP-sensitive K+ channel blocker)

Propafenone Hydrochloride (β-adrenergic antagonist, Kv1.4 and K2P2 K+ channel blocker)

Protopanaxatriol (GABA-A/C antagonist, slow-activating delayed rectifier K+ channel blocker)

Repaglinide (ATP-sensitive K+ channel blocker)

Rhyncholphylline (hERG K+ and L-type Ca2+ channel channel blocker, NMDA antagonist)

Ritodrine Hydrochloride (β2-adrenergic agonist, SK/BK and ATP-sensitive K+ channel activator)

Sarafotoxin 6c (ET-B agonist, ATP-sensitive K+ channel activator)

Simvastatin (HMG-CoA reductase inhibitor, potential ATP-sensitive K+ channel activator, L-type Ca2+ channel blocker)

Sotalol Hydrochloride (β-adrenergic antagonist, voltage-gated Na+ and K+ channel blocker)

Speract (K+ channel activator, speract SRCR agonist)

Tetrahydroberberine (5-HT1A agonist, D2 antagonist, ATP-sensitive K+ channel blocker)

D,L-Tetrahydropalmatine (D1/2 antagonist, potential L-type Ca2+ and K+ channel blocker)

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)

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

Trimebutine Base (BK K+ channel and L-type Ca2+ channel blocker)

Trimebutine Maleate (L-type Ca2+ channel blocker, BK K+ channel modulator, potential opioid agonist)

Troglitazone (PPARγ agonist, ATP-sensitive K+ channel blocker)

Tyrphostin A25 (SK K+ channel blocker, EGFR inhibitor)

Verruculogen (BK K+ channel blocker, GABA-A antagonist)

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

Voglibose (α-glucosidase inhibitor, potential GLP-1 agonist, potential ATP-sensitive K+ channel activator)

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)

Dantrolene Sodium Heptahydrate (RyR antagonist, L-type Ca2+ channel blocker)

Mitiglinide Calcium (ATP-sensitive K+ channel blocker, potential RyR agonist)

Suramin Hexasodium (RyR agonist, SIRT, telomerase, P2Y, GPCR inhibitor)

Aconitine (voltage-gated Na+ channel modulator)

Amiloride Hydrochloride Dihydrate (ENaC and acid-sensing ion channel blocker, Na+/H+ antiporter inhibitor)

Amiodarone Hydrochloride (Voltage-gated Na+, Ca2+, K+ channel blocker, α/β-adrenergic antagonist, FIASMA)

Brevetoxin 2 (Nav1.4/1.5 Na+ channel activator)

Brevetoxin 3 (Nav1.4/1.5 Na+ channel activator)

Bulleyaconitine A (voltage-gated Na+ channel blocker)

Bupivacaine (BK/SK, Kv1, Kv3, TASK-2 K+ channel blocker, voltage-gated Na+ channel blocker)

Bupivacaine Hydrochloride Monohydrate (voltage-gated Na+, BK/SK, Kv1, Kv3, TASK-2 K+ channel inhibitor)

Carbamazepine (voltage-gated Na+ and ATP-sensitive K+ channel blocker)

Clonidine Hydrochloride (Imidazoline and α2-adrenergic agonist, Nav1.7 Na+ channel blocker)

Dihydromethysticin (Voltage-gated Na+ and L-type Ca2+ channel blocker)

Diphenhydramine Hydrochloride (Voltage-gated Na+ channel blocker, mAChR antagonist, histamine H1 inverse agonist)

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

Flufenamic Acid (TREK1 K+ potentiator, voltage-gated Na+ channel blocker, TRPC3 and TRPM2 antagonist, COX-1/2 inhibitor)

Hypaconitine (voltage-gated Na+ channel modulator)

Imperatorin (voltage-gated Na+ channel blocker, AChE and BChE inhibitor)

Kawain (Voltage-gated Na+ and L-type Ca2+ channel blocker)

Lamotrigine (R-type Ca2+ and voltage-gated Na+ channel blocker)

Lappaconitine (cardiac Na+ channel blocker)

Oxcarbazepine (α4β2 nAChR desensitizer, delayed-rectifier voltage-gated K+ and voltage-gated Na+ channel blocker)

Penicillic Acid (BK K+, voltage-gated cardiac Na+, K+, Ca2+ channel inhibitor)

Proxymetacaine Hydrochloride (Potential voltage-gated Na+ channel blocker)

Ranolazine Dihydrochloride (Nav1.7 and Nav1.8 N1+ channel blocker)

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

Sotalol Hydrochloride (β-adrenergic antagonist, voltage-gated Na+ and K+ channel blocker)

Terbutaline (β2-adrenergic agonist, potential ENaC activator)

Trifluoperazine Dihydrochloride (D1/2 and α1-adrenergic antagonist, calmodulin and CDPK4 inhibitor, Nav1.4 and Nav1.7 Na+ channel blocker)

Valproic Acid Sodium (T-type Ca2+ and voltage-gated Na+ channel blocker, GABA transaminase and HDAC inhibitor)

Zonisamide (carbonic anhydrase inhibitor, voltage-gated Na+ and T-type Ca2+ channel blocker)

D,L-1′-Acetoxychavicol Acetate (TRPA1 agonist, xanthine oxidase inhibitor)

Arvanil (CB1 agonist, TRPV1 agonist)

AS-252424 (p110γ PI3K inhibitor, potential TRPC1/5/6 negative modulator, potential TRPC3/7 positive modulator)

Azelastine Hydrochloride (TRPV1 agonist, histamine H1 antagonist)

Capsaicin, natural (TRPV agonist)

Carveol (TRPV3 agonist)

Cromolyn Sodium (potential TRP antagonist, potential Cl- channel blocker)

Etodolac (TRPA1 agonist, COX-2 inhibitor)

Flufenamic Acid (TREK1 K+ potentiator, voltage-gated Na+ channel blocker, TRPC3 and TRPM2 antagonist, COX-1/2 inhibitor)

Ginsenoside Rc (AMPK inhibitor, potential TRPV1 antagonist)

Ginsenoside Rd (26S proteasome inhibitor, TRPM7 antagonist)

(+)-Ketanserin Tartrate (5-HT2A and TRPV1 antagonist, potential α1-adrenergic antagonist)

Lomerizine Dihydrochloride (L-type and T-type Ca2+ and TRP antagonist)

Methyl Salicylate (TRPV1 modulator)

Neomycin Sulfate (protein translation inhibitor, cation channel/receptor (P2X, TRPV1) blocker)

Nocistatin (TRPC agonist, BK/SK K+ channel modulator)

Parthenolide (TRPA1 partial agonist, NLRP3 and caspase 1 inhibitor)

Peimine (TRPV1 and TRPA1 antagonist)

Peiminine (M2 mAChR antagonist, potential TRPV1 and TRPA1 antagonist)

Pimecrolimus (Calcineurin inhibitor, potential TRPV1 agonist)

Piperine (TRPV1 agonist)

Pregnenolone (TRPM3 agonist, NMDA potentiator, GABA-A negative allosteric modulator)

Resiniferatoxin (PKC and TRPV agonist)

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

Sumatriptan Succinate (5-HT1B/1D agonist, TRPV1 antagonist)

Tranilast (TRPV2 antagonist, PDGFR inhibitor)

Zerumbone (potential TRPV1 antagonist)