SCH-221510 explained

SCH-221510 is an experimental opioid drug. It has potential as an analgesic and as a treatment to addiction of certain drugs.

Mechanism of action

Most opioid analgesics act through delta, mu, and kappa opioid receptors; however, SCH-221510 is instead an agonist at the nociceptin receptor.

Analgesic effects

Classical opioid analgesics (such as morphine) usually have effects such as constipation, hypoventilation and addiction.^[1] However, by acting through a different receptor, SCH-221510 seems to be lacking the undesirable effects of morphine at equianalgesic doses.^[2] This suggests that SCH-221510 could be a better opioid than the currently available opioid pain medications, by having less side effects.

Treatment of drug addiction

SCH-221510 might be an option in the treatment of certain drug addictions: it is able to decrease ethanol self-administration^[3] and was able to decrease self-administration of remifentanil, a fentanyl analogue, in a study,^[4]

Notes and References

1. Nakatani . Toshihiko . April 2017 . [Opioid Therapy and Management of Side Effects Associated with Opioids] . Gan to Kagaku Ryoho. Cancer & Chemotherapy . 44 . 4 . 294–297 . 0385-0684 . 28428507.
2. Lin . Ann P. . Ko . Mei-Chuan . 2012-10-24 . The Therapeutic Potential of Nociceptin/Orphanin FQ Receptor Agonists as Analgesics without Abuse Liability . ACS Chemical Neuroscience . 4 . 2 . 214–224 . 10.1021/cn300124f . 1948-7193 . 3582300 . 23421672.
3. Flynn . Shawn M. . Epperly . Phillip M. . Davenport . April T. . Cami-Kobeci . Gerta . Husbands . Stephen M. . Ko . Mei-Chuan . Czoty . Paul W. . July 2019 . Effects of stimulation of mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors on alcohol drinking in rhesus monkeys . Published online: 10 April 2019 . Neuropsychopharmacology . 44 . 8 . 1476–1484 . 10.1038/s41386-019-0390-z . free . 1740-634X . 6784996 . 30970376.
4. Sukhtankar . Devki D. . Lagorio . Carla H. . Ko . Mei-Chuan . 2014-12-15 . Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats . European Journal of Pharmacology . 745 . 182–189 . 10.1016/j.ejphar.2014.10.029 . 1879-0712 . 4259829 . 25446568.