Applications: A multi-faceted invention that has identified novel compositions that may be useful for pharmacological, diagnostic and research development for more effective pain control. An in vitro enzymatic process that produces novel glucuronyl derivatives of cannabinoids. This work serves as the basis for broader application of this class of enzymatic modifications.
Cannabinoid - any of the chemical compounds that are the active principles of marijuana.
Glucuronide – a glycoside that yields glucuronic acid upon hydrolysis.
Researchers have demonstrated that specific human glucuronosyltransferases (UGTs) are responsible for the synthesis of cannabinoid glucuronides (CG) in vivo and that human recombinant UGTs can be used to produce glucuronides of classical cannabinoids. Based on studies with other pain control compounds these derivatives may provide more potent and less toxic forms of pain therapeutics. For example, glucuronyl derivatives of morphine such as 6-0-morphine glucuronide are 800 fold more active than morphine itself. Therefore, cannabinoid glucuronides, which show very close structural and biological activities, are anticipated to have enhanced activity. Identification of biological activity of different cannabinoid glucuronides will have important clinical and pharmacological application in pain management.
Additionally, this invention includes diagnostic methods for the identification of cannabinoid glucuronides. These methods can be used for the quantitative analysis of these glucuronides in urine and plasma and potentially allow for them to serve as new biomarkers for identification of cannabinoids in human body tissues. These therapeutic compounds can be manufactured in significant quantities, and methods to prepare labeled standards are also possible.
The present patent addresses the fact that little information currently exists on the synthesis and characterization of specific cannabinoid glucuronides by human enzymes. This area of glucuronidation both chemical and enzymatic is currently under development.
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09-23 (D, T, E) Radominska-Pandya