CGS-8216

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CGS-8216.svg

Chemical compound


CGS-8216
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CGS-8216 is a chemical compound that acts as a benzodiazepine receptor antagonist. It is known for its ability to counteract the effects of benzodiazepines, which are a class of drugs primarily used for treating anxiety, insomnia, and several other conditions.

Pharmacology

CGS-8216 binds to the GABA A receptor at the same site as benzodiazepines but does not activate the receptor. Instead, it blocks the effects of benzodiazepines, making it useful in research to study the role of GABA A receptors in various physiological and pathological processes.

Mechanism of Action

The primary mechanism of action of CGS-8216 involves its interaction with the GABA A receptor. By binding to the benzodiazepine site on the receptor, CGS-8216 prevents benzodiazepines from exerting their effects, which include sedation, anxiolysis, and muscle relaxation. This makes CGS-8216 a valuable tool in the study of GABAergic neurotransmission.

Research Applications

CGS-8216 is widely used in neuroscience research to investigate the role of GABA A receptors in the central nervous system. It has been employed in studies examining the effects of benzodiazepines on memory, anxiety, and seizures. Additionally, CGS-8216 has been used to explore the potential therapeutic applications of benzodiazepine receptor antagonists in conditions such as benzodiazepine overdose and dependence.

Safety and Toxicity

As with many research chemicals, the safety and toxicity profile of CGS-8216 is not fully understood. It is primarily used in controlled laboratory settings, and its effects in humans have not been extensively studied. Researchers handling CGS-8216 should follow appropriate safety protocols to minimize any potential risks.

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Contributors: Prab R. Tumpati, MD