Date published: 2026-3-19

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SB 612111 hydrochloride (CAS 371980-98-2 (free base))

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Alternate Names:
(5S,7S)-7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride
Application:
SB 612111 hydrochloride is a piperidine derivative shown to act as a selective NOP (KOR-3) receptor antagonist
CAS Number:
371980-98-2 (free base)
Molecular Weight:
454.86
Molecular Formula:
C24H29Cl2NO•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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SB 612111 hydrochloride, a selective antagonist of the orexin-1 receptor (OX1R), plays a role in regulating wakefulness and arousal. This receptor, a G-protein coupled receptor, is associated with various physiological processes such as feeding behavior, energy metabolism, and stress responses. Over time, SB 612111 hydrochloride has become useful for investigating the involvement of the orexin system in these processes. By blocking the activity of the orexin system, SB 612111 hydrochloride acts as a selective antagonist, inhibiting its effects on these physiological processes.


SB 612111 hydrochloride (CAS 371980-98-2 (free base)) References

  1. Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).  |  Zaratin, PF., et al. 2004. J Pharmacol Exp Ther. 308: 454-61. PMID: 14593080
  2. Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vivo studies.  |  Rizzi, A., et al. 2007. J Pharmacol Exp Ther. 321: 968-74. PMID: 17329551
  3. Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vitro studies.  |  Spagnolo, B., et al. 2007. J Pharmacol Exp Ther. 321: 961-7. PMID: 17329552
  4. Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice.  |  Khroyan, TV., et al. 2011. J Pharmacol Exp Ther. 339: 687-93. PMID: 21859931
  5. Acute and chronic antiparkinsonian effects of the novel nociceptin/orphanin FQ receptor antagonist NiK-21273 in comparison with SB-612111.  |  Marti, M., et al. 2013. Br J Pharmacol. 168: 863-79. PMID: 22994368
  6. The biology of Nociceptin/Orphanin FQ (N/OFQ) related to obesity, stress, anxiety, mood, and drug dependence.  |  Witkin, JM., et al. 2014. Pharmacol Ther. 141: 283-99. PMID: 24189487
  7. Spinal antinociceptive effects of the novel NOP receptor agonist PWT2-nociceptin/orphanin FQ in mice and monkeys.  |  Rizzi, A., et al. 2015. Br J Pharmacol. 172: 3661-70. PMID: 25828800
  8. The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor.  |  Miller, RL., et al. 2015. Structure. 23: 2291-2299. PMID: 26526853
  9. Genetic and pharmacological evidence that endogenous nociceptin/orphanin FQ contributes to dopamine cell loss in Parkinson's disease.  |  Arcuri, L., et al. 2016. Neurobiol Dis. 89: 55-64. PMID: 26804029
  10. Buprenorphine requires concomitant activation of NOP and MOP receptors to reduce cocaine consumption.  |  Kallupi, M., et al. 2018. Addict Biol. 23: 585-595. PMID: 28635181
  11. Role of mu-opioid agonist efficacy on antinociceptive interactions between mu agonists and the nociceptin opioid peptide agonist Ro 64-6198 in rhesus monkeys.  |  Cornelissen, JC., et al. 2019. Eur J Pharmacol. 844: 175-182. PMID: 30552903
  12. Potent and selective NOP receptor activation reduces cocaine self-administration in rats by lowering hedonic set point.  |  Cippitelli, A., et al. 2020. Addict Biol. 25: e12844. PMID: 31709687
  13. Fear expression is reduced after acute and repeated nociceptin/orphanin FQ (NOP) receptor antagonism in rats: therapeutic implications for traumatic stress exposure.  |  Taylor, RM., et al. 2020. Psychopharmacology (Berl). 237: 2943-2958. PMID: 32588078
  14. Antinociceptive Efficacy of the µ-Opioid/Nociceptin Peptide-Based Hybrid KGNOP1 in Inflammatory Pain without Rewarding Effects in Mice: An Experimental Assessment and Molecular Docking.  |  Dumitrascuta, M., et al. 2021. Molecules. 26: PMID: 34071603
  15. Synthesis, Biological Activity and Molecular Docking of Chimeric Peptides Targeting Opioid and NOP Receptors.  |  Wtorek, K., et al. 2022. Int J Mol Sci. 23: PMID: 36293553

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

SB 612111 hydrochloride, 5 mg

sc-361347
5 mg
$128.00

SB 612111 hydrochloride, 25 mg

sc-361347A
25 mg
$510.00