SCH-221510

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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.[1]

Analgesic effects

Classical opioid analgesics (such as morphine) usually have effects such as constipation, hypoventilation and addiction.[2] However, by acting through a different receptor, SCH-221510 seems to be lacking the undesirable effects of morphine at equianalgesic doses.[1] 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]

References

  1. 1.0 1.1 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. doi:10.1021/cn300124f. ISSN 1948-7193. PMID 23421672. 
  2. Nakatani, Toshihiko (April 2017). "[Opioid Therapy and Management of Side Effects Associated with Opioids]". Gan to Kagaku Ryoho. Cancer & Chemotherapy 44 (4): 294–297. ISSN 0385-0684. PMID 28428507. 
  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". Neuropsychopharmacology 44 (8): 1476–1484. doi:10.1038/s41386-019-0390-z. ISSN 1740-634X. PMID 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. doi:10.1016/j.ejphar.2014.10.029. ISSN 1879-0712. PMID 25446568. 




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