Ion Channel

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.

Peripheral vasodilator; nootropic agent

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.

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.

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.

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.

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.

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.

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.

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.

Gardos channel inhibitor