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Potent NK1 receptor antagonist (Ki = 0.74 nM. IC50 = 1.6 nM). Inhibits substance P-invoked calcium mobilization and outward current (IC50 = 1.3 nM); blocks NK1-mediated nitric oxide-dependent vasodilation in vivo.
|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 656.12. 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||1.52 mL||7.62 mL||15.24 mL|
|5 mM||0.3 mL||1.52 mL||3.05 mL|
|10 mM||0.15 mL||0.76 mL||1.52 mL|
|50 mM||0.03 mL||0.15 mL||0.3 mL|
References are publications that support the biological activity of the product.
Hall and Brain (1994) Inhibition by SR140333 of NK1 tachykinin receptor-evoked, nitric oxide-dependent vasodilation in the hamster cheek pouch microvasculature in vivo. Br.J.Pharmacol. 113 522 PMID: 7530573
Nieuwmeyer et al (2006) Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of Caj J.Pharmacol.Exp.Ther. 317 439 PMID: 16330493
Oury-Donat et al (1994) SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line. J.Neurochem. 62 1399 PMID: 7510780
Emonds-Alt et al (1993) In vitro and in vivo biological activities of SR140333, a novel non-peptide tachykinin NK1 receptor antagonist. Eur.J.Pharmacol. 250 403 PMID: 7509286
If you know of a relevant reference for SR 140333, please let us know.
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Keywords: SR 140333, SR 140333 supplier, SR140333, neurokinin1, nk1, tachykinins, receptor, antagonists, potent, NK1, Receptor, 4012, 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.
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.