Description:
Background

Cannabinoid receptors have been shown to play an important role in many areas of human physiology and are useful in treatment or potential treatment of several human medical conditions. Cannabinoid receptor agonists are already in use as treatments for chemotherapy-induced nausea, spasticity in patients with multiple sclerosis, and appetite enhancers for patients with HIV/AIDS or undergoing chemotherapy.

 

More recently there has been intense interest in the therapeutic properties of drugs that act as antagonists at CB1. However, some of these compounds have drawbacks which are caused by down-regulation of the receptor leading to a reduction in efficacy and reversal of weight loss on cessation of treatment, and the CNS effects, which includes suicidal thought, nausea, and depression.

 

The present application relates to the synthetic derivatives which are negative allosteric modulators of the cannabinoid 1 (CB1) receptor and are useful in the treatment of several diseases including neuropathic pain, cancer, obesity as well as neuropathic pain and inflammation. This application is also directed towards the synthesis of the covalent probes for the allosteric site of the CB1 receptors which will help map the binding site through LAPS (Ligand Assisted Protein Structure) approach followed by Mass Spectrometry studies. 
 
Technology Overview
This invention suggests that the toxicological issues associated with cannabinoid antagonism could be eliminated by a drug tuned down excessive receptor activation, rather than turned it off completely. This effect can be achieved by the use of allosteric modulators and the therapeutic potential of cannabinoid receptor modulation harnesses without the associated side effects of global activation or inhibition of the receptor.
 
Benefits
- Molecules can be used as diagnostic tools and also for analytical purposes in CB1 allosterism 
- Helps in treatment of neuropathic pain and inflammation
- Targets allosteric sites
- Has high specificity for allosteric sites
 
Applications
- Neuopathic diseases
- Pharmaceuticals
- Allosteric Therapeutics
- Mapping Allosteric sites
- Treatment of CB! mediated disorders
 
Opportunity
- Research Collaboration
- partnering
- License
 
Patent Information:
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Ganeshsingh Thakur
Pushkar Kulkarni
Abhijit Kulkarni
Ritesh Tichkule
Keywords:
Chemistry
Drug Discovery & Development
Health
Pharmaceutical Composition