PK 11195

PK 11195 is a chemical compound that acts as a selective antagonist of the peripheral benzodiazepine receptor (PBR), also known as the translocator protein (TSPO). This compound is widely used in scientific research to study the function and distribution of TSPO in various biological systems.

Chemical Structure

Chemical structure of PK 11195

PK 11195 is a isoquinoline carboxamide derivative. Its chemical structure is characterized by a core isoquinoline ring system, which is crucial for its binding affinity to the TSPO. The presence of specific functional groups in its structure allows it to interact selectively with the TSPO, distinguishing it from other benzodiazepine receptors.

Mechanism of Action

PK 11195 functions primarily as an antagonist of the TSPO. The TSPO is a protein located on the outer mitochondrial membrane and is involved in the transport of cholesterol into mitochondria, a critical step in the synthesis of steroid hormones. By binding to TSPO, PK 11195 can inhibit or modulate its activity, which is useful in studying the role of TSPO in various physiological and pathological processes.

Applications in Research

PK 11195 is extensively used in neuroscience and oncology research. In neuroscience, it is employed to investigate the role of TSPO in neuroinflammation and neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. In oncology, PK 11195 is used to study the expression of TSPO in various types of cancer cells, as TSPO is often upregulated in tumor tissues.

Neuroimaging

PK 11195 is also used in positron emission tomography (PET) imaging to visualize TSPO expression in the brain. Radiolabeled forms of PK 11195, such as [11C]PK 11195, are used as tracers to detect areas of neuroinflammation in vivo, providing valuable insights into the progression of neurological disorders.

Pharmacological Properties

PK 11195 exhibits high affinity for the TSPO, with minimal activity at central benzodiazepine receptors. This selectivity makes it a valuable tool for distinguishing between the functions of peripheral and central benzodiazepine receptors in various tissues.

Limitations and Challenges

While PK 11195 is a powerful research tool, its use is not without limitations. The compound's binding affinity and selectivity can vary across different species, which may affect the interpretation of experimental results. Additionally, the development of more selective and potent TSPO ligands is an ongoing area of research, aiming to overcome some of the limitations associated with PK 11195.

Related Pages

• Translocator protein
• Neuroinflammation
• Positron emission tomography
• Isoquinoline