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Selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. Inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo following i.v. and oral administration.
Sold with the permission of Astellas Pharma Inc.
|Storage||Store at -20°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 588.69. 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||1.7 mL||8.49 mL||16.99 mL|
|5 mM||0.34 mL||1.7 mL||3.4 mL|
|10 mM||0.17 mL||0.85 mL||1.7 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References are publications that support the biological activity of the product.
Fujii et al (1992) Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist. Br.J.Pharmacol. 107 785 PMID: 1282073
Murai et al (1993) Effects of an NK1 receptor antagonist, FK888, on constriction and plasma extravasation induced in guinea pig airway by neurokinins and capsaicin. Eur.J.Pharmacol. 236 7 PMID: 7686493
Aramori et al (1994) Subtype- and species-selectivity of a tachykinin receptor antagonist, FK888, for cloned rat and human tachykinin receptors. Eur.J.Pharmacol. 269 277 PMID: 7531648
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Keywords: FK 888, FK 888 supplier, High, affinity, NK1, receptor, antagonists, Tachykinin, Receptors, Neurokinin, FK888, Receptor, 2400, Tocris Bioscience
1 Citation for FK 888
Citations are publications that use Tocris products. Selected citations for FK 888 include:
Mondal et al (2013) Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons. PLoS One 8 e60365 PMID: 23565235
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.