New fluorinated DREADD actuators and ligands suitable for PET imaging

Unmet Need
Chemogenetics is defined as a method by which proteins are made to interact with small molecules, typically neurological molecules, as they have never been interacted with before. There is a powerful and versatile approach for remote and momentary manipulation of cellular activity called Designer Receptors Exclusively Activated by Designer Drugs (DREADD). Mutated human muscarinic receptors are activated by this “designer drug” rather than other typical neurotransmitters. Currently, there exists needs for improvement in DREADD methods and compositions, specifically there is a need for new compounds directed to treating diseases and disorders in subjects. These subjects have currently only amounted to lab animals, and there is a need to delve into clinical testing. Chemogenetics has the potential to have a large research and eventual clinical impact, because engineered proteins can have enormous implications on overall health.
 
Technology Overview
The inventors have proposed multiple new compounds and a new methodology to be applied to this DREADD method. Their invention provides compounds that consist of a pharmaceutical composition along with a pharmaceutically acceptable carrier. In addition, they have also proposed a method that can utilize these compounds to effect a GPCR-mediated response as a method to treat diseases or disorders. This hinges on their method for administering this pharmaceutically acceptable salt (any of their proposed compounds) to the subject. This method and new compounds will allow for further chemogenetic neurological manipulation with more efficiency, accuracy, and an overall movement towards clinical applications.
 
Stage of Development
The inventors have created prototypes for their compounds and have performed tests to determine the accuracy and effectiveness of their new method of “designer drug” delivery. They have received grant money through NIH and are continuing their research. 
 

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