Ion Channel

<p>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.</p>

<p>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.<br>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&amp;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.</p>

<p>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.</p>

<p>Antagonist of purine receptor P2Y1</p>

<p>Resiniferatoxin is a natural chemical found in some plants that activates pain receptors.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Calcium channel blocker</p>

<p>Partial agonist of α4β2 nicotinic receptors; acetylcholine receptor α7 agonist</p>

<p>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).<br>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&amp;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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Clinidipine is a dihydropyridine calcium channel blocker that is used to treat hypertension. This drug acts on L-type calcium channels of blood vessels by blocking calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. . Cilnidipine also shows activity against N-type calcium channels.</p>

<p>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.</p>

<p>Lamotrigine is an antiepileptic phenyltriazine drug that is used to treat epilepsy and as a mood stabilizer in bipolar disorder. Although, this drug’s action is not fully well understood it is similar to carbamazepine which involves inhibiting voltage-sensitive sodium channels. Lamotrigine blocks voltage-sensitive sodium channels, which reduces neuronal excitability by blocking action potentials.</p>

<p>Positive allosteric modulator of GABA(A) receptor</p>

<p>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.</p>

<p>L-type calcium channel blocker</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Minoxidil is an antihypertensive agent used for the treatment of resistant hypertension that has caused organ damage. This drug has vasodilatory properties and promotes the survival of human dermal papillary cells. Therefore, this drug is also used to treat alopecia.</p>

<p>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.</p>

<p>Vanilloid receptor 1 antagonist</p>

<p>Potassium channel blocker; antiarrhythmic agent</p>

<p>GABAA receptor antagonist that displaces [3H]-GABA in membranes of rat brain (Ki value 0.15 µM). Has greater affinity for GABAA than bicuculline (20-fold greater). Inhibits Cl- current induced by GABA, but not pentobarbitone. Low-affinity inhibitor of glycine receptors.</p>

<p>Voltage-dependent K+ channel opener; insulinotropic sulfonylurea receptor ligand</p>

<p>Oxcarbazepine metabolite; anticonvulsant; sodium channel blocker</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Aminosteroid; neuromuscular blocker in anaesthetics</p>

<p>Acamprosate is a drug that has been shown to have a synergic effect in the treatment of alcohol dependence. It is a structural analogue of the neurotransmitter gamma-aminobutyric acid (GABA). Acamprosate works by binding to glutamate receptors and inhibiting the release of glutamate, which may help restore the balance between excitatory and inhibitory neurotransmitters in the brain. Acamprosate also has a protective effect on brain cells by inhibiting protein synthesis and increasing the production of glutathione, which acts as an antioxidant.</p>

<p>AR-R 17779 is a selective agonist for α7 nicotinic acetylcholine receptors or nAChRs. It is suggested that AR-R 17779 reduces formation of atherosclerotic plaques and abdominal aortic aneurysms in apolipoprotein E-deficient mice.</p>

<p>Antagonist of NMDA glutamate receptor at glycine binding site</p>

<p>Potassium channel blocker; anti-arrhythmic; cardiac depressant</p>

<p>Benidipine is a synthetic dihydropyridine calcium channel blocker. This drug is used in the treatment of coronary heart diseases, hypertension, and angina pectoris. Benipidine binds to the L-type voltage-gated calcium channels and blocks their opening which leads to smooth muscle relaxation and a decrease in blood pressure.</p>

<p>Inhibits cardiac late sodium channel current; antiarrhythmic</p>

<p>Nicotinic receptor antagonist</p>

<p>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.</p>

<p>Sodium channel blocker; anti-arrhythmic agent</p>

<p>Inhibitor of TASK tandem pore potassium channel; respiratory stimulant</p>

<p>Antagonist of serotonin receptors 5-HT3</p>