Invention:
This invention is a dynorphin analog designed to interact with a receptor that is partly responsible for pain sensations. Dynorphin analog targets the bradykinin receptors instead of the f NMDA receptors. The ligands are novel in the deletion of an arginine residue in position 7 which has been recognized as an essential residue for opioid and non-opioid activities. This deletion has been shown to retain biological activity for the receptor. The researchers have also identified the minimum pharmacophore (combination of more than 2 basic amino acids and 2 hydrophobic amino acids) for the bradykinin receptor.
Applications:
- Use as an analgesic, specifically analgesia against chronic pain
- Another potential application for this invention is use as an anti-inflammatory drug
- There is a possibility, that with little to no modification. This particular dynorphin analog can be used to treat mild inflammation
- Has potential application in pain modulation and analgesia
Advantages:
- The dynorphin analog targets a different pathway, bradykinin receptors instead of NMDA receptors, to offer pain relief without the standard side effects
- The series of dimorphic A analogs show therapeutic benefit to modulate pain, since it has been shown that up-regulation of dynorphin causes hyperalgesia by interacting with the bradykinin receptor
Status: issued U.S. patent #10,428,115
