Ion Channel

<p>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.</p>

<p>Natural neurotoxin</p>

<p>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.</p>

<p>Inhibitor of TRPC6 cation channel</p>

<p>NMDA glutamate receptor antagonist</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>NMDA glutamate receptor antagonist</p>

<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>