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Submit ReviewSB 612111 hydrochloride
Description: Selective NOP antagonist
Chemical Name: (5S,7S)-7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride
Purity: ≥97% (HPLC)
Biological Activity for SB 612111 hydrochloride
SB 612111 hydrochloride is a selective NOP receptor antagonist (Ki values are 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively). Antagonizes the pronociceptive action of nociceptin (Cat. No. 0910) in an acute pain model. Potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries for SB 612111 hydrochloride
SB 612111 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 612111 hydrochloride
| M. Wt | 454.86 |
| Formula | C24H29Cl2NO.HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| PubChem ID | 21061234 |
| InChI Key | DCKUVQADDNMWEF-DQFHVVJASA-N |
| Smiles | CC1=CC=CC2=C1CC[C@H](CN3CCC(C4=C(Cl)C=CC=C4Cl)CC3)C[C@@H]2O.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 612111 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.49 | 100 | |
| ethanol | 22.74 | 50 |
Preparing Stock Solutions for SB 612111 hydrochloride
The following data is based on the product molecular weight 454.86. 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 | 2.2 mL | 10.99 mL | 21.98 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.4 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for SB 612111 hydrochloride
References for SB 612111 hydrochloride
References are publications that support the biological activity of the product.
Zaratin et al (2004) Modification of nociception and mor. 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) J.Pharmacol.Exp.Ther. 308 454 PMID: 14593080
Rizzi et al (2007) 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. J.Pharmacol.Exp.Ther. 321 968 PMID: 17329551
Spagnolo et al (2007) 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. J.Pharm.Exp.Ther. 106 961
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Keywords: SB 612111 hydrochloride, SB 612111 hydrochloride supplier, SB612111, hydrochloride, opioids, NOP, receptors, antagonists, ORL1, N/OFQ, 371980-98-2, Receptors, 3573, Tocris Bioscience
2 Citations for SB 612111 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 612111 hydrochloride include:
Michael R et al (2019) Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists. Sci Signal 12 PMID: 30914485
Hardaway et al (2016) Nociceptin receptor antagonist SB 612111 decreases high fat diet binge eating. Behav Brain Res 307 25 PMID: 27036650
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.