PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural

nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ner ...

s, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...

. It reduces

excitotoxicity In excitotoxicity, nerve cells suffer damage or death when the levels of otherwise necessary and safe neurotransmitters such as glutamate become pathologically high, resulting in excessive stimulation of receptors. For example, when glutamate ...

and protects striatal dopaminergic neurons in rat models. It also potentiates cognitive enhancement from

memantine Memantine is a medication used to slow the progression of moderate-to-severe Alzheimer's disease. It is taken by mouth. Common side effects include headache, constipation, sleepiness, and dizziness. Severe side effects may include blood clots ...

, decreases dynorphin release and inhibits GSK-B3.

References

{{Nicotinic acetylcholine receptor modulators Nicotinic agonists Stimulants Quinuclidines Carboxamides Furopyridines

See also

References