PNU-282,987

PNU-282,987.svg

PNU-282,987 is a selective agonist for the α7 nicotinic acetylcholine receptor (α7 nAChR). It is a synthetic compound that has been widely used in scientific research to study the role of α7 nAChR in various physiological and pathological processes.

Chemical Properties

PNU-282,987 is a small molecule with the chemical formula C_14H_18N_2O. It is known for its high affinity and selectivity towards the α7 nAChR, making it a valuable tool in neuropharmacology.

Mechanism of Action

As an agonist of the α7 nAChR, PNU-282,987 binds to this receptor and mimics the action of the endogenous neurotransmitter acetylcholine. The α7 nAChR is a ligand-gated ion channel that, when activated, allows the flow of cations such as sodium and calcium into the cell. This leads to various downstream effects, including the modulation of neurotransmitter release and the regulation of intracellular signaling pathways.

Research Applications

PNU-282,987 has been extensively used in research to investigate the role of α7 nAChR in the central nervous system (CNS). Studies have shown that α7 nAChR is involved in cognitive processes such as learning and memory, and PNU-282,987 has been used to explore its potential therapeutic effects in neurodegenerative diseases like Alzheimer's disease.

Neuroprotection

Research has indicated that activation of α7 nAChR by PNU-282,987 can have neuroprotective effects. This has been particularly relevant in models of stroke and traumatic brain injury, where PNU-282,987 has been shown to reduce neuronal damage and improve functional outcomes.

Anti-inflammatory Effects

PNU-282,987 has also been studied for its anti-inflammatory properties. Activation of α7 nAChR on immune cells can inhibit the release of pro-inflammatory cytokines, making PNU-282,987 a compound of interest in the study of inflammatory diseases.

Potential Therapeutic Uses

Given its effects on the CNS and immune system, PNU-282,987 is being investigated for its potential therapeutic applications in a variety of conditions, including schizophrenia, Alzheimer's disease, and inflammatory bowel disease.

Safety and Toxicity

While PNU-282,987 has shown promise in preclinical studies, its safety and toxicity profile in humans is not well-established. Further research is needed to determine its potential side effects and long-term safety.

Conclusion

PNU-282,987 is a potent and selective agonist of the α7 nAChR, with significant implications for research in neuropharmacology and immunology. Its ability to modulate cognitive functions and inflammatory responses makes it a valuable tool for scientific investigation and a potential candidate for therapeutic development.

See Also

• α7 nicotinic acetylcholine receptor
• Agonist
• Neuropharmacology
• Alzheimer's disease
• Inflammatory diseases