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Submit ReviewSCH 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). Exhibits anxiolytic-like activity at doses that have no effect on overt behaviors such as locomotion in vivo. Orally active.
SCH 221510 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 397.55 |
公式 | C28H31NO |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 322473-89-2 |
PubChem ID | 9887077 |
InChI Key | LOSJNRBXNQTUNT-UHFFFAOYSA-N |
Smiles | OC1(C2=CC=CC=C2)CC3N(C(C5=CC=CC=C5C)C4=C(C)C=CC=C4)C(CC3)C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.76 | 100 |
以下数据基于产品分子量 397.55。 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: SCH 221510, SCH 221510 supplier, SCH221510, NOP, nociceptin, opioid, receptors, agonists, ORL1, Receptors, 3240, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SCH 221510 的部分引用包括:
Wu & Liu (2018) ORL1 activation mediates a novel ORL1 receptor agonist SCH221510 analgesia in neuropathic pain in rats. J Mol Neurosci 66 10 PMID: 30074175
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.