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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.

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.

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.

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.

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.

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.

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.