Ion Channel

Prilocaine is a drug used as a local anaesthetic in dental procedures. It has been shown to reduce the incidence of pain caused. This drug is also a sodium channel blocker that blocks the influx of sodium into cells.

Icilin is a transient receptor potential M8 (TRPM8) agonist drug that is used for the treatment of pruritis. This drug has shown to be effective in producing an extreme cold sensation in both human and animal models. It is used in research for studying TRP channels.

Nifedipine is a dihydropyridine calcium channel blocker that is used to manage several subtypes of angina pectoris and hypertension. This drug blocks L-type voltage gated calcium channels in order for blood pressure to be reduced and an increase in oxygen supply to the heart.

L-type calcium channel blocker

Ambroxol is a secretolytic agent that is used in the treatment of respiratory diseases and chronic coughs. Ambroxol has been shown to inhibit the NO-dependent activation of soluble guanylate cyclase so that the airway is not inflamed or its functions are not disturbed. Also, excessive mucus secretion is suppressed which as a result lowers the phlegm viscosity.

Agonist of kainate receptors, a subclass of ionotropic glutamate receptors with neuroexcitatory action. At high concentrations, it can induce seizures and act as neurotoxin, causing neuron death due to overstimulation.

Mibefradil is a calcium channel antagonist with the highest selectivity for T- and L-type channels, but also effective for N-, Q-, and R-type calcium channels at micromolar range. It decreases smooth muscle proliferation in response to vascular injury and causes vessel dilatation.

Amantadine is an antiviral drug that is used to treat dyskinesia in patients with Parkinson’s disease. This drug’s mechanism is not fully understood however it is said to aid in releasing dopamine from the nerve ending in brain cells. Amantadine is also an NDMA antagonist.

Positive allosteric modulator of GABA(A) receptor

Felodipine is a calcium channel blocker and a member of the 1,4-dihydropyridine class of calcium channel blockers that is used to treat high blood pressure and related conditions. Felodipine increases the level of natriuretic peptide in the blood and reduces levels of infectious diseases such as influenza A virus and respiratory syncytial virus (RSV). Felodipine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Partial agonist of α4β2 nicotinic receptors; acetylcholine receptor α7 agonist

Piracetam is a nootropic drug that is used for the treatment of sickle cell disease, alcohol dependence and as a cognitive enhancer. This drug is a cyclic derivative of GABA and has neuroprotective and anticonvulsant properties. Piracetam has been said to improve neuronal plasticity.

Activates CFTR channels

NAP is a neuroprotective peptide, which is derived from activity-dependent neuroprotective protein (ADNP), with a mechanism involving microtubule stabilization and neuronal protection. It exhibits the ability to protect neurons from various types of damage, including oxidative stress and conditions mimicking neurodegenerative diseases. NAP enhances axonal transport and increases the resilience of neurons to insults that would typically result in cell death. This peptide has shown promise in preclinical studies for its potential to halt or reverse cognitive decline, making it a focal point for research into therapeutic strategies for disorders like Alzheimer's disease and other tauopathies. The peptide operates by binding to microtubules, promoting stability, and facilitating efficient transport of cellular components. Studies have highlighted its role in traversing the blood-brain barrier, which makes it a viable candidate for central nervous system-targeted therapies. Researchers continue to explore its efficacy and possible applications in improving cognitive function and providing neuroprotection in aging populations.

NMDA receptor antagonist

Competitive antagonist of ionotropic glutamate receptors of AMPA and kainate subfamilies. Reported anti-convulsant activity in seizures models induced by electrostimulation, drugs or genetic predisposition. Pro-convulsant effects in Theiler's murine encephalomyelitis virus-induced (TMEV) seizure model.

Nateglinide is used to treat type 2 diabetes mellitus as an oral hypoglycemic, insulinotropic agent. It is a blocker of ATP-dependent potassium channels and works by increasing the body's production of insulin, which lowers blood glucose levels. Nateglinide has been shown to be effective in reducing postprandial blood glucose levels in patients with type 2 diabetes who have not responded well to other treatments. The effects of nateglinide are reversible.

Flupirtine is a pyridine derivative that is used as a non-opioid analgesic. Flupirtine promotes Bcl-2, raises glutathione levels, activates an inward rectifying potassium channel, and reverses the effect of calcium on neuronal cell death by inhibiting its release from intracellular stores. Although it doesn't attach to the receptor, flupirtine functions as an NMDA receptor antagonist. It is used for the treatment of fibromyalgia.

A selective P2X7 receptor antagonist with an IC50 value of 11.2 nM. Prevents breast cancer resistance protein (BCRP)-mediated transport of methotrexate. Has therapeutic potential for osteoarthritis due to its anti-proliferative and pain-relieving effects.

AR-R 17779 is a selective agonist for α7 nicotinic acetylcholine receptors (nAChRs) (Ki value = 190 nM for rat α7 receptor). This compound has use as a tool to study the function of α7 nicotinic receptors. One such study revealed a role for α7 nicotinic receptors in nicotine-mediated excitatory effects on hippocampal learning and memory. AR-R17779 reduces formation of atherosclerotic plaques and abdominal aortic aneurysms in apolipoprotein E-deficient mice.

Ondansetron is a serotonin 5-HT3 receptor antagonist that has been shown to inhibit the effects of serotonin in the gastrointestinal tract, thereby preventing nausea and vomiting that is caused by cancer chemotherapy. Chemotherapy and radiotherapy are associated with the release of serotonin (5-HT) from enterochromaffin cells of the small intestine, initiating a vomiting reflex through stimulation of 5-HT3 receptors located on vagal afferents. Ondansetron blocks the initiation of this reflex. The drug binds to receptors on cells in the gastrointestinal tract that are normally activated by serotonin, thereby blocking its effect.

Calcium channel blocker

Peripheral vasodilator; nootropic agent

Ondansetron is a serotonin 5-HT3 receptor antagonist that is used to prevent vomiting and nausea in patients undergoing chemotherapy. This drug blocks the initiation of the vomiting reflex.

Nicardipine is calcium channel blocker drug that is used for the treatment of hypertension and angina. This drug can also be used in the treatment of asthma and is said to enhance the action of various antineoplastic agents.

Gardos channel inhibitor

Verapamil is drug that belongs to the class of drugs known as calcium channel blockers. It is used to treat high blood pressure, angina and other cardiovascular disorders. It works by relaxing the blood vessels so that blood can flow more easily. It does this by inhibiting the calcium ion influx through slow channels into conductile, contractile myocardial cells and vascular smooth muscle cells.

Lercanidipine is a calcium channel blocker that is used for the treatment of hypertension. This drug inhibits ion channels and interferes with the release of calcium from the sarcoplasmic reticulum. As a result, coronary and systemic arteries are dilated, allowing for an increased supply of oxygen to myocardial tissue. .

Flunarizine is calcium channel blocker that helps to reduce muscle spasms. It shows antimigraine and anticonvulsive activity. This occurs by inhibiting the influx of extracellular calcium through myocardial and vascular membrane pores by physically inhibiting the voltage-dependent calcium channels. Additionally, this drug is a D2 dopamine receptor antagonist.

Tocainide is a class 1b antiarrhythmic agent that is used in the treatment of ventricular arrhythmias. This drug acts on sodium channels to decrease the excitability of myocardial cells. This drug also prevents the depolarization of cardiac muscle cells and prolongs their refractory period.

Natural neurotoxin

Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.

Lacidipine is a lipophilic dihydropyridine calcium channel blocker that is used in the treatment of hypertension. This drug acts as an antihypertensive agent to dilate peripheral arteries and reduces blood pressure. Lacidipine blocks voltage-dependent L-type calcium channels.

Inhibitor of TRPC6 cation channel

NMDA glutamate receptor antagonist

Nisoldipine is a calcium channel blocker that is used to treat hypertension. It acts on vascular smooth muscle cells by blocking voltage-gated L-type calcium channels. By inhibiting the influx of calcium in smooth muscle cells, Nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction.

Selective partial GABAA receptor antagonist of subtypes  α1, α2, α3, α5 subunits. Non-sedative anxiolytic effects demonstrated in vivo, without compromising motor activity. Anti-nociceptive and anti-inflammatory activities also demonstrated in vivo.

Ivabradine is a HCN channel blocker that is used to reduce the risk of hospitalization for worsening heart failure and used in the treatment of symptomatic heart failure. This drug acts by inhibiting the “funny” channel pacemaker current (If) which results in a lower heart rate and allows for more blood flow to the myocardium.

Inhibitor of the transient receptor vanilloid channel, specific for the TRPV2 subtype with IC50 value of 0.46 μM. In human prostate cancer cells, SET2 inhibited cell migration but did not affect cell survival. SET2 has been proposed as a potential anti-cancer and anti-metastatic agent.

NMDA glutamate receptor antagonist

Palonosetron is a selective serotonin 5-HT3 receptor antagonist. It is an antinauseant and antiemetic agent that has been shown to be effective in preventing nausea and vomiting induced by cancer chemotherapy, radiotherapy, or surgery. By directly inhibiting serotonin activity in the region postrema and the chemoreceptor trigger zone, the inhibition of 5-HT3 receptors also prevents the visceral afferent stimulation of the vomiting center.

Amiodarone, a class III anti-arrhythmic agent is 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 diarrhoea. Amiodarone HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

A type-II positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors with IC50 values of 216 nM. Increases calcium flux in response to agonists, by lengthening the channel’s mean open time. Ex vivo and in vivo models of ischemic stroke demonstrate the conversion of endogenous choline or acetylcholine into neuroprotective agents by PNU 120596.

Sparteine hydroiodide is the salt form of sparteine. This compound acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.

Picrotoxin is a GABA-A receptor antagonist that is used to relieve respiratory distress. This drug also is used as an antidote from poisoning by CNS depressants. Picrotoxin works by blocking the GABA activated chloride ionophore.

Repaglinide is an antihyperglycemic drug that is used for the improvement of glycemic control in diabetes. This drug acts on the beta cells of the pancreas and binds to specific receptors on the beta cells known as ATP-sensitive potassium channels. As a result, this promotes insulin secretion from beta cells.