Targeted Agonist Provides Analgesia Without Typical Side Effects

Researchers from The Scripps Research Institute (TSRI), Florida campus, report their discovery of a novel drug candidate for the treatment of pain and itch that both reduces the potential for abuse associated with opioid narcotics and avoids the common side effects of other kappa opioid receptor (KOR) agonists. The new candidate, triazole 1.1, is a “biased” KOR agonist, and was favorably compared to a conventional KOR agonist in rodent models in the new study. Senior author Laura Bohn, PhD, professor in the department of molecular therapeutics at TSRI commented, “The most significant aspect of the study is that we can preserve itch and pain treatment qualities in a KOR agonist that we developed—triazole 1.1—while avoiding the euphoria associated with narcotic opioids and the dysphoria associated with some other selective KOR agonists.” The findings were published last week online in Science Signaling.

KOR agonists have been shown to be effective in treating chronic pain and itch, and do not produce the abuse-provoking “high” associated with opioids that target other receptors. However, they also reduce the body’s level of dopamine, causing dysphoria and sedation, and these side effects have limited their therapeutic utility. But the new candidate, triazole 1.1, appears to preferentially activate some pathways over others, avoiding the sedative and dysphoric effects while preserving analgesic efficacy.

Read more about the study here.

The journal abstract may be read here.

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