Ion Channel

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Piracetam analog; AMPA receptor allosteric modulator</p>

<p>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.</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>NMDA receptor antagonist</p>

<p>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.</p>

<p>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.</p>

<p>NMDA glutamate receptor antagonist; anti-depressant</p>

<p>5-HT3 receptor antagonist; alpha-7 nicotinic acetylcholine receptor partial agonist</p>

<p>Activates CFTR channels</p>

<p>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.</p>

<p>NMDA receptor antagonist</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>