Potent neuropeptide S receptor (NPSR) antagonist (pA2 = 9.98). Inhibits neuropeptide S-induced ERK phosphorylation over cAMP responses and calcium responses (IC50 values are 9.3, 22.1 and 36.5 nM, respectively). Appears to modulate addictive behavior in vivo. Displays no activity against vasopressin V1B receptors. Brain penetrant.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 545.47. 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||1.83 mL||9.17 mL||18.33 mL|
|5 mM||0.37 mL||1.83 mL||3.67 mL|
|10 mM||0.18 mL||0.92 mL||1.83 mL|
|50 mM||0.04 mL||0.18 mL||0.37 mL|
References are publications that support the biological activity of the product.
Patnaik et al (2013) Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor. J Med Chem. 56 9045 PMID: 24171469
Thorsell et al (2013) A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats. J.Neurosci. 33 10132 PMID: 23761908
If you know of a relevant reference for ML 154, please let us know.
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Keywords: ML 154, ML 154 supplier, ML154, Potent, selective, Neuropeptide, S, receptors, NPSR, antagonists, ERK, phosphorylation, additive, behaviour, Blood, brain, barrier, permeable, Receptors, 5161, Tocris Bioscience
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