Ion Channel

Antagonist of NMDA glutamate receptor at glycine binding site

Inhibits cardiac late sodium channel current; antiarrhythmic

Voltage-dependent K+ channel opener; insulinotropic sulfonylurea receptor ligand

Oxcarbazepine metabolite; anticonvulsant; sodium channel blocker

Amlodipine is a calcium channel blocker that is used to treat hypertension and angina. This drug inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle.

Amiodarone a class III anti-arrhythmic agent, used to treat and prevent certain types of irregular heartbeats. It is a competitor for natural ligands of alpha and beta adrenergic receptors, muscarinic acetylcholine receptors, histamine H1 receptors, and serotonin 5HT2A/5HT2C receptors. Amiodarone has been shown to reduce the number of atrial and ventricular arrhythmias in patients with structural heart disease, and has been used to treat atrial fibrillation, ventricular tachycardia, and Wolff-Parkinson-White Syndrome. It has also been used in the prevention of myocardial infarcts due to its ability to modify blood pressure and maintain cardiac function. In addition, amiodarone inhibits prostaglandin synthesis by inhibiting cyclooxygenase enzymes. This prevents inflammation in the gastrointestinal tract and reduces bowel disease symptoms such as cramping or diarrhea.

Piracetam analog; AMPA receptor allosteric modulator

Resiniferatoxin is a natural chemical found in some plants that activates pain receptors.

Flumazenil is a drug that reverses the effects of benzodiazepines, such as diazepam, lorazepam, and midazolam. It binds to the α1 subunit of the GABA receptor and prevents it from opening. Flumazenil is a benzodiazepine antagonist.

NMDA glutamate receptor antagonist; anti-depressant

Vinpocetin or Vinpocetine is a synthetic derivative of a vinca alkaloid that is used to treat symptoms of cerebrovascular diseases such as stroke and dementia. It blocks sodium channels, reduces cellular calcium influx and has shown to have antioxidant activity. Studies have also suggested that vinpocetin can inhibit phosphodiesterase- 1 (PDE-1) in isolated rabbit aorta.

Cytisine is an alkaloid found in plants derived from the Fabaceae family. It has partial agonist activity at the α4β2 nicotinic acetylcholine receptor used to aid smoking cessation. Recent studies have shown it to be a more effective smoking cessation treatment than nicotine replacement therapy.

Riluzole is a glutamate antagonist that is used for the treatment of amyotrophic lateral sclerosis. This drug is also used as an anticonvulsant. Although a complete mechanism of action is unknown, it has an inhibitory effect on glutamate release and it inactivates voltage dependent sodium channels.

Suzetrigine is a novel compound classified as a synthetic ligand, which is derived through advanced chemical synthesis techniques. This compound engages specific targets within biological systems, acting primarily as a selective modulator of ion channels.

Sparteine acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.

Sodium channel inhibitor; inhibitor of urokinase-type plasminogen activator

Oxcarbazepine is an anti-epileptic drug that is used for the treatment of partial-onset seizures. Although, the mechanism of action for this drug is unclear, it is said to involve the blockage of voltage-gated sodium channels. As a result, the firing of the action potentials which lead to seizures are reduced and so seizure activity is inhibited.

NBQX is a competitive antagonist of ionotropic glutamate receptors of AMPA and kainate subfamilies. It has been reported anti-convulsant activity in seizures models induced by electrostimulation, drugs or genetic predisposition. It has also exhibited pro-convulsant effects in Theiler's murine encephalomyelitis virus-induced (TMEV) seizure model.

NMDA receptor antagonist

Bicuculline is a phthalide-isoquinoline compound and is a competitive GABA receptor antagonist. It blocks GABA’s inhibitory action, mimicking epilepsy. This compound is used in research to better study epilepsy.

5-HT3 receptor antagonist; alpha-7 nicotinic acetylcholine receptor partial agonist

Selective TRPM8 channel blocker. Inhibits icillin-induced store-operated Ca2+ entry, hence TRPM8 activation, in pulmonary vasculature. Reduces frequency of volume-induced contraction of bladder. Reduces micturition and nociceptive reflex actions in the bladder, suggesting therapeutic potential for bladder hypersensitivity disorders.

Aniracetam is a nootropic drug that is used to alleviate memory disturbances caused by cerebrovascular disease and brain disorders. This drug has anti-depressive and anxiolytic properties and is said to target serotonin and dopamine receptors.

Glimepiride is a sulfonylurea drug that is used in the treatment of type 2 diabetes mellitus. This drug works by inhibiting ATP-sensitive potassium channels by binding non-specifically to the B sites of both sulfonylurea receptor-1 (SUR1) and sulfonylurea receptor-2A (SUR2A) subunits. As a result, this promotes insulin secretion from beta cells.

Antagonist of nicotinic acetylcholine receptors; nondepolarising muscle relaxant

Carbamazepine is an anticonvulsant that is used to treat epilepsy and nerve pain from trigeminal neuralgia. The mechanism of action for Carbamazepine is not well understood but it is theorized that carbamazepine reduces seizure activity by preventing sodium channel activation. This interaction reduces the frequency and duration of sodium channel opening, slowing down nerve impulses and helping to prevent seizures Studies on animals have shown that carbamazepine works by reducing polysynaptic nerve response and preventing post-tetanic potentiation.

Antagonist of purine receptor P2Y1

Nicorandil is an ATP-dependent potassium channel activator. It activates mitochondrial ATP-dependent potassium (KATP) channels and inhibits the TLR4/MyD88/NF-κB/NLRP3 pathway, which reduces myocardial infarction-induced pyroptosis. Pyroptosis is an inflammatory cell death process that regulates cardiomyocyte loss after myocardial infarction. These findings suggest that nicorandil may be a potential therapy for ischemic heart disease due to its cardioprotective effects.

Aloe-emodin is an anthraquinone derivative that is found in the aloe plant. It has a strong stimulant laxative action. Aloe-emodin may be useful in the treatment of cancer, as it inhibits cell proliferation by inducing apoptosis.