SCH 221510 | CAS# 322473-89-2 | NOP Agonist

MedKoo Cat#: 532692 | Name: SCH 221510

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SCH 221510 is a potent and selective nociceptin opioid receptor (NOP) agonist (EC50 values are 12, 693, 683 and 8071 nM, and Ki values are 0.3, 65, 131 and 2854 nM at NOP, μ-, κ- and δ-opioid receptors respectively). SCH221510 exhibits anxiolytic-like activity at doses that have no effect on overt behaviors such as locomotion in vivo.

Chemical Structure

SCH 221510

CAS#322473-89-2

Theoretical Analysis

MedKoo Cat#: 532692

Name: SCH 221510

CAS#: 322473-89-2

Chemical Formula: C28H31NO

Exact Mass: 397.2406

Molecular Weight: 397.56

Elemental Analysis: C, 84.59; H, 7.86; N, 3.52; O, 4.02

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 405.00	2 Weeks
50mg	USD 1,395.00	2 Weeks

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Related CAS #

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Synonym

SCH221510; SCH 221510; SCH-221510.

IUPAC/Chemical Name

8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol

InChi Key

LOSJNRBXNQTUNT-UHFFFAOYSA-N

InChi Code

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

SMILES Code

OC1(C2=CC=CC=C2)CC(N3C(C4=CC=CC=C4C)C5=CC=CC=C5C)CCC3C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Biological target:

SCH 221510 is an NOP agonist (EC50 values are 12, 693, 683 and 8071 nM, and Ki values are 0.3, 65, 131 and 2854 nM at NOP, μ-, κ- and δ-opioid receptors respectively).

In vitro activity:

To be determined

In vivo activity:

SCH 221510 may have potential in the treatment of drug addiction. When given to rodents, SCH 221510 did not prompt the same response to self-administer the drug as the traditional opioid remifentanil. Instead, SCH 221510 curbed the desire for remifentanil, similar to naltrexone. Unlike naltrexone, SCH221510 reduced the rodents' motivation to seek non-drug rewards, like sucrose pellets. Reference: Eur J Pharmacol. 2014 Dec 15;745:182-9. https://pubmed.ncbi.nlm.nih.gov/25446568/

	Solvent	mg/mL	mM
Solubility
	DMSO	39.8	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 397.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Sukhtankar DD, Lagorio CH, Ko MC. Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats. Eur J Pharmacol. 2014 Dec 15;745:182-9. doi: 10.1016/j.ejphar.2014.10.029. Epub 2014 Oct 29. PMID: 25446568; PMCID: PMC4259829. 2. Sobczak M, Mokrowiecka A, Cygankiewicz AI, Zakrzewski PK, Sałaga M, Storr M, Kordek R, Małecka-Panas E, Krajewska WM, Fichna J. Anti-inflammatory and antinociceptive action of an orally available nociceptin receptor agonist SCH 221510 in a mouse model of inflammatory bowel diseases. J Pharmacol Exp Ther. 2014 Mar;348(3):401-9. doi: 10.1124/jpet.113.209825. Epub 2013 Dec 17. PMID: 24345466.

In vitro protocol:

To be determined

In vivo protocol:

1: Islam A, Rahman MA, Brenner MB, Moore A, Kellmyer A, Buechler HM, DiGiorgio F, Verchio VR, McCracken L, Sumi M, Hartley R, Lizza JR, Moura-Letts G, Fischer BD, Keck TM. Abuse Liability, Anti-Nociceptive, and Discriminative Stimulus Properties of IBNtxA. ACS Pharmacol Transl Sci. 2020 Jul 27;3(5):907-920. doi: 10.1021/acsptsci.0c00066. PMID: 33073190; PMCID: PMC7551712. 2: Flynn SM, Epperly PM, Davenport AT, Cami-Kobeci G, Husbands SM, Ko MC, Czoty PW. Effects of stimulation of mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors on alcohol drinking in rhesus monkeys. Neuropsychopharmacology. 2019 Jul;44(8):1476-1484. doi: 10.1038/s41386-019-0390-z. Epub 2019 Apr 10. PMID: 30970376; PMCID: PMC6784996. 3: Ferrari F, Malfacini D, Journigan BV, Bird MF, Trapella C, Guerrini R, Lambert DG, Calo' G, Zaveri NT. In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403. Pharmacol Res Perspect. 2017 Aug;5(4):e00333. doi: 10.1002/prp2.333. PMID: 28805972; PMCID: PMC5684865. 4: Agostini S, Petrella C. The endogenous nociceptin/orphanin FQ-NOP receptor system as a potential therapeutic target for intestinal disorders. Neurogastroenterol Motil. 2014 Nov;26(11):1519-26. doi: 10.1111/nmo.12460. PMID: 25307525. 5: Kothandan G, Gadhe CG, Balupuri A, Ganapathy J, Cho SJ. The nociceptin receptor (NOPR) and its interaction with clinically important agonist molecules: a membrane molecular dynamics simulation study. Mol Biosyst. 2014 Dec;10(12):3188-98. doi: 10.1039/c4mb00323c. Epub 2014 Sep 26. PMID: 25259728. 6: Fichna J, Sobczak M, Mokrowiecka A, Cygankiewicz AI, Zakrzewski PK, Cenac N, Sałaga M, Timmermans JP, Vergnolle N, Małecka-Panas E, Krajewska WM, Storr M. 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. Neurogastroenterol Motil. 2014 Nov;26(11):1539-50. doi: 10.1111/nmo.12390. Epub 2014 Jul 15. PMID: 25041572. 7: Sobczak M, Mokrowiecka A, Cygankiewicz AI, Zakrzewski PK, Sałaga M, Storr M, Kordek R, Małecka-Panas E, Krajewska WM, Fichna J. Anti-inflammatory and antinociceptive action of an orally available nociceptin receptor agonist SCH 221510 in a mouse model of inflammatory bowel diseases. J Pharmacol Exp Ther. 2014 Mar;348(3):401-9. doi: 10.1124/jpet.113.209825. Epub 2013 Dec 17. PMID: 24345466. 8: Witkin JM, Statnick MA, Rorick-Kehn LM, Pintar JE, Ansonoff M, Chen Y, Tucker RC, Ciccocioppo R. The biology of Nociceptin/Orphanin FQ (N/OFQ) related to obesity, stress, anxiety, mood, and drug dependence. Pharmacol Ther. 2014 Mar;141(3):283-99. doi: 10.1016/j.pharmthera.2013.10.011. Epub 2013 Nov 1. Erratum in: Pharmacol Ther. 2014 Sep;143(3):351. PMID: 24189487; PMCID: PMC5098338. 9: Cremeans CM, Gruley E, Kyle DJ, Ko MC. Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates. J Pharmacol Exp Ther. 2012 Oct;343(1):72-81. doi: 10.1124/jpet.112.194308. Epub 2012 Jun 28. PMID: 22743574; PMCID: PMC3464037. 10: Varty GB, Lu SX, Morgan CA, Cohen-Williams ME, Hodgson RA, Smith-Torhan A, Zhang H, Fawzi AB, Graziano MP, Ho GD, Matasi J, Tulshian D, Coffin VL, Carey GJ. 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). J Pharmacol Exp Ther. 2008 Aug;326(2):672-82. doi: 10.1124/jpet.108.136937. Epub 2008 May 20. PMID: 18492950.