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). Exhibits anxiolytic-like activity at doses that have no effect on overt behaviors such as locomotion in vivo. Orally active.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 397.55. Batch specific molecular weights may vary from batch to batch due to solvent 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||2.52 mL||12.58 mL||25.15 mL|
|5 mM||0.5 mL||2.52 mL||5.03 mL|
|10 mM||0.25 mL||1.26 mL||2.52 mL|
|50 mM||0.05 mL||0.25 mL||0.5 mL|
References are publications that support the biological activity of the product.
Varty et al (2008) 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. 326 672 PMID: 18492950
Lambert (2008) The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential. Nat.Rev.Drug Discov. 7 694 PMID: 18670432
Yang et al (2009) Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety. Bioorg.Med.Chem.Lett. 19 2482 PMID: 19332374
If you know of a relevant reference for SCH 221510, please let us know.
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Keywords: SCH 221510, SCH 221510 supplier, SCH221510, NOP, nociceptin, opioid, receptors, agonists, ORL1, Receptors, 3240, Tocris Bioscience
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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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.