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SCH-221510

From Wikipedia, the free encyclopedia
Nociceptin receptor agonist
SCH-221510
Names
IUPAC name
(1S,5R)-8-[Bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
  • InChI=1S/C28H31NO/c1-20-10-6-8-14-25(20)27(26-15-9-7-11-21(26)2)29-23-16-17-24(29)19-28(30,18-23)22-12-4-3-5-13-22/h3-15,23-24,27,30H,16-19H2,1-2H3/t23-,24+,28?
    Key: LOSJNRBXNQTUNT-XUEDKKMFSA-N
  • CC1=CC=CC=C1C(C2=CC=CC=C2C)N3[C@@H]4CC[C@H]3CC(C4)(C5=CC=CC=C5)O
Properties
C28H31NO
Molar mass397.562 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

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

[edit]

Most opioid analgesics act throughdelta,mu, andkappa opioid receptors; however, SCH-221510 is instead anagonist at thenociceptin receptor.[1]

Analgesic effects

[edit]

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 atequianalgesic 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

[edit]

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 ofremifentanil, a fentanyl analogue, in a study,[4]

References

[edit]
  1. ^abLin, 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.PMC 3582300.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) [Published online: 10 April 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.PMC 6784996.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.PMC 4259829.PMID 25446568.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others
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