Molecular structure of SCH 221510, CAS Number: 322473-89-2
SCH 221510 (CAS 322473-89-2)
Alternate Names:
3-Endo-8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol
Application:
SCH 221510 is A potent and selective nociceptin opiod receptor (KOR-3) agonist.
CAS Number:
322473-89-2
Molecular Weight:
397.55
Molecular Formula:
C28H31NO
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SCH 221510 is a novel high-efficacy, piperidine-based, selective and potent nociceptin opioid receptor (NOP), which is coded by the same gene as KOR-3 receptor, agonist, (EC50 values are 12, 693, 683 and 8071 nM, and Ki values are 0.3, 65, 131 and 2854 nM at NOP, mu-, kappa- and delta-opioid receptors respectively). The nociceptin opioid receptor plays a role in the modulation of pain, stress, anxiety, appetite, and reward systems in the brain. The NOP receptor interacts with its endogenous peptide, nociceptin/orphanin FQ. SCH 221510 also exhibits anxiolytic-like activity.
SCH 221510 (CAS 322473-89-2) References
- The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510). | Varty, GB., et al. 2008. J Pharmacol Exp Ther. 326: 672-82. PMID: 18492950
- The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential. | Lambert, DG. 2008. Nat Rev Drug Discov. 7: 694-710. PMID: 18670432
- Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety. | Yang, SW., et al. 2009. Bioorg Med Chem Lett. 19: 2482-6. PMID: 19332374
- Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. | Thompson, AA., et al. 2012. Nature. 485: 395-9. PMID: 22596163
- Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates. | Cremeans, CM., et al. 2012. J Pharmacol Exp Ther. 343: 72-81. PMID: 22743574
- Anti-inflammatory and antinociceptive action of an orally available nociceptin receptor agonist SCH 221510 in a mouse model of inflammatory bowel diseases. | Sobczak, M., et al. 2014. J Pharmacol Exp Ther. 348: 401-9. PMID: 24345466
- Activation of the endogenous nociceptin system by selective nociceptin receptor agonist SCH 221510 produces antitransit and antinociceptive effect: a novel strategy for treatment of diarrhea-predominant IBS. | Fichna, J., et al. 2014. Neurogastroenterol Motil. 26: 1539-50. PMID: 25041572
- The nociceptin receptor (NOPR) and its interaction with clinically important agonist molecules: a membrane molecular dynamics simulation study. | Kothandan, G., et al. 2014. Mol Biosyst. 10: 3188-98. PMID: 25259728
- The endogenous nociceptin/orphanin FQ-NOP receptor system as a potential therapeutic target for intestinal disorders. | Agostini, S. and Petrella, C. 2014. Neurogastroenterol Motil. 26: 1519-26. PMID: 25307525
- Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor. | Chang, SD., et al. 2015. Mol Pharmacol. 88: 502-11. PMID: 26134494
- In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403. | Ferrari, F., et al. 2017. Pharmacol Res Perspect. 5: PMID: 28805972
- Effects of stimulation of mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors on alcohol drinking in rhesus monkeys. | Flynn, SM., et al. 2019. Neuropsychopharmacology. 44: 1476-1484. PMID: 30970376
- Abuse Liability, Anti-Nociceptive, and Discriminative Stimulus Properties of IBNtxA. | Islam, A., et al. 2020. ACS Pharmacol Transl Sci. 3: 907-920. PMID: 33073190
Activator of:
DOR, KOR-3, and MOR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SCH 221510, 10 mg | sc-358790 | 10 mg | $363.00 | |||
| US: Only available in the US | ||||||
SCH 221510, 50 mg | sc-358790A | 50 mg | $1566.00 | |||
| US: Only available in the US | ||||||