Available Technology

Radiotracers for Imaging P-glycoprotein Transporter Function

This invention offers technology to help treat certain brain diseases, such as Alzheimer's disease and Parkinson's, and may lead to more effective and personalized treatments. P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established/prospective chemotherapeutics (a phenomenon known as multidrug resistance; MDR). The instant invention relates to compounds that are avid substrates for P-gp, and their preparation and use as radiotracers for imaging P-gp function in vitro and in vivo.
Abstract: 
This invention offers technology to help treat certain brain diseases, such as Alzheimer's disease and Parkinson's, and may lead to more effective and personalized treatments. P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established/prospective chemotherapeutics (a phenomenon known as multidrug resistance; MDR). The instant invention relates to compounds that are avid substrates for P-gp, and their preparation and use as radiotracers for imaging P-gp functionin vitroandin vivo.
Benefits: 
This class of radiotracer, typified by the described [11C]dLop, is designed to restrict the formation of radiometabolites that would obstruct the measurement of P-gp function at the blood-brain barrier or at tumors. In this sense these radiotracers are vastly superior to progenitors (e.g. [11C]verapamil, [11C]loperamide), which can only give qualitative not quantitative information.
applications: 
Inventors: 

Robert Innis (NIMH)

Neva Lazarous (NIMH)

Sami Zoghbi (NIMH)

Victor Pike (NIMH)

Patent Number: 
7,989,630issued 2011-08-02
Internal Laboratory Ref #: 
E-318-2007/0 Updated: Nov 9, 2015
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