Description:
Background
Radiochemical methods have been in use for more than twenty years for studying the complex phenomena associated with the endocannabinoid system and cannabinergic molecules. Despite the usefulness of radiochemical methods, the use of alternative methods such as fluorescent techniques and nitroxide spin labeling technologies can provide information not readily accessible by conventional radiochemical methods and circumvent certain drawbacks associated with them, such as high cost, special precautions in handling and disposal, and potential health hazards.
 
Technology Overview
The present invention provides novel cannabinoid ligands that modulate cannabinoid(CB) receptors. The foremost unusual feature of the invented compounds over existing cannabinoid ligands is that the invented compounds carry imaging/diagnostic or therapeutic functional groups. These functional groups include fluorescent groups, nitroxide spin labels, biotin moieties, and groups with enhanced polarity. Usually, incorporation of such functional groups into the structure of cannabinoid compounds leads to a severe reduction of the binding affinity of the compound for the CB1/CB2 receptors. Surprisingly, many invented compounds in this disclosure exhibit remarkably high affinities (Ki = 0.01-10 nM) for the cannabinoid CB1 and CB2 receptors. This phenomenon is extremely rare not only for cannabinoid receptors but also for the large family of all G-protein-coupled receptors. Northeastern University researchers have successfully applied the so-called “click” technology toward linking a large variety of functional groups with the classical cannabinoid framework. The “click” technology links two chemical structures/moieties via the formation of the enzymatically stable and polar triazole ring in aqueous reaction conditions, and it is compatible with a plethora of functional groups and biological systems.
 
Benefits
- Fluorescent cannabinergic ligands can exhibit higher labeling efficiency and higher selectivity for the CB1 and CB2 receptors over other proteins. 
- The cannabinergic ligands in addition to carrying imaging/diagnostic groups they also exhibit the ability to bind tightly/irreversibly to cannabinoid receptors. This allows imaging using such ligands for extended periods. 
 
Applications
- Can be used as in vivo imaging agents for the early diagnosis of diseases that are related to up- or down-regulation of cannabinoid receptors (for example diabetes and cancer).
- Can be used as research tools to study the complex pharmacology of these proteins using biochemical, bioanalytical, and biophysical methods.
- Can be useful to address the high lipophilicity issue.
 
Opportunity
- License
- Partnering
- Research collaboration
Patent Information:
Category(s):
Diagnostics
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Alexandros Makriyannis
Spyridon Nikas
Christos Iliopoulos Tsoutsouvas
Shashank Kulkarni
Lipin Ji
Keywords:
Cannabinoids
Chemistry
Diagnostics
Drug Discovery & Development
Drugs
Imaging
MRI contrast agent
Single-molecule mapping
Therapeutic