A-582,941

A-582,941

A-582,941 is a chemical compound that acts as a selective agonist for the α7 subtype of the nicotinic acetylcholine receptor (nAChR). This compound has been the subject of research due to its potential therapeutic applications in neurological disorders, particularly those involving cognitive deficits such as Alzheimer's disease and schizophrenia.

Chemical Structure and Properties

A-582,941 is a small molecule with the following chemical structure:

- IUPAC Name: 1-(5-chloro-2-pyridinyl)-3-(4-pyridinyl)-1H-pyrazole - Molecular Formula: C14H9ClN4 - Molecular Weight: 268.7 g/mol

The compound is characterized by its pyrazole core, which is substituted with pyridinyl groups, one of which is chlorinated. This structure is crucial for its activity as an α7 nAChR agonist.

Mechanism of Action

A-582,941 functions by selectively binding to and activating the α7 nicotinic acetylcholine receptors. These receptors are ligand-gated ion channels that, when activated, allow the flow of cations such as calcium and sodium into the neuron. This influx of ions leads to depolarization and subsequent neuronal activation.

The α7 nAChR is predominantly expressed in the central nervous system, particularly in regions associated with cognitive processing such as the hippocampus and prefrontal cortex. Activation of these receptors is thought to enhance synaptic plasticity and improve cognitive function.

Therapeutic Potential

Research into A-582,941 has primarily focused on its potential to ameliorate cognitive deficits. Studies in animal models have shown that A-582,941 can improve performance in tasks that require attention and memory. These findings suggest that α7 nAChR agonists like A-582,941 could be beneficial in treating conditions such as:

- Alzheimer's Disease: By enhancing cholinergic signaling, A-582,941 may help counteract the cognitive decline associated with Alzheimer's. - Schizophrenia: Cognitive impairments are a core feature of schizophrenia, and α7 nAChR agonists may help improve these symptoms.

Research and Development

While A-582,941 has shown promise in preclinical studies, its development as a therapeutic agent is still ongoing. Challenges such as optimizing its pharmacokinetic properties and ensuring its safety and efficacy in humans remain.

Also see

- Nicotinic acetylcholine receptor - Cognitive enhancers - Alzheimer's disease - Schizophrenia