Protein Complex May Be Alternative to Opioid Pain Relievers

Researchers believe that a drug that targets a protein complex containing two different types of opioid receptors may be an effective alternative to morphine and other opioid pain medications, minus the harsh, addictive side effects often associated with opioid medications.

According to researchers at the lcahn School of Medicine at Mount Sinai, they identified a therapeutic target called a GPCR heteromer, which is a protein complex made up of two opioid receptors called mu and delta. They also showed that the heteromer is abundant in the area of the brain the processes pain, and is likely the cause of morphine tolerance and side effects.

Lead study author Lakshmi Devi, Professor of Pharacology and Systems Therapeutics, carried out high throughput screening in collaboration with researchers at the National Institutes of Health (NIH) to help identify which small molecules might act on the signaling pathway associated with the protein complex.

According to the study, researchers discovered that one compound called CYM51010 was as potent as morphine but not as likely to result in tolerance and negative side effects. The researchers are still currently developing modified versions of this compound that may have the potential to reduce side effects, as noted via the study.

"GPCR heteromers have been suggested to represent powerful targets for improved, novel therapeutics with reduced adverse effects in people with severe pain," said Dr. Devi, via a press release. "However, there are presently no chemical tools that allow us to investigate their role in vivo. Our work represents a promising step in this direction, providing results that pave the way towards a new understanding of the function and pharmacology of opioid receptor heteromers."

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More information regarding the study can be found in the journal Proceedings of the National academy of Sciences.