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Potent NK1 antagonist (Ki values are 0.08, 0.2 and 93.13 nM for gerbil, human and rat receptors, respectively). Produces anxiolytic-like effects in the gerbil elevated plus-maze. Exhibits antitumor activity in vitro. Also decreases HER2 activity and tumor growth in mice bearing HER2+ or EGFR+ breast tumors. Orally bioavailable and brain penetrant.
Sold with the permission of Merck, Sharpe and Dohme Ltd.
|Storage||Store at RT|
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|
|water||21.99||50 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 439.83. 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|
|0.5 mM||4.55 mL||22.74 mL||45.47 mL|
|2.5 mM||0.91 mL||4.55 mL||9.09 mL|
|5 mM||0.45 mL||2.27 mL||4.55 mL|
|25 mM||0.09 mL||0.45 mL||0.91 mL|
References are publications that support the biological activity of the product.
Kramer et al (1998) Distinct mechanism for antidepressant blockade of central substance P receptors. Science 281 1640 PMID: 9733503
Seabrook et al (1996) L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur.J.Pharmacol. 317 129 PMID: 8982729
Varty et al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371 PMID: 12225694
Garcia-Recio et al (2013) Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer. Cancer Res. 73 6424 PMID: 24030979
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Keywords: L-733,060 hydrochloride, L-733,060 hydrochloride supplier, Potent, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L733060, Receptor, 1145, Tocris Bioscience
15 Citations for L-733,060 hydrochloride
Citations are publications that use Tocris products. Selected citations for L-733,060 hydrochloride include:
Fong et al (2017) The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1. PLoS One 12 e0174101 PMID: 28301610
Backman et al (2014) Substance P reduces TNF-α-induced apoptosis in human tenocytes through NK-1 receptor stimulation. Mol Cancer Res 48 1414 PMID: 23996004
Liu et al (2013) TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J 27 3549 PMID: 23722916
Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. PLoS One 294 R1517 PMID: 18337316
Muschter et al (2019) Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages. Int J Mol Sci 20 PMID: 30682804
Zhang et al (2008) Sprouting of substance P-expressing primary afferent central terminals and spinal micturition reflex NK1 receptor dependence after spinal cord injury. Am J Physiol Regul Integr Comp Physiol 295 R2084 PMID: 18945947
Khasabov et al (2017) Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla. J Neurophysiol 118 2727 PMID: 28794197
D'Amato et al (2015) A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer. Cancer Res 75 4651 PMID: 26363006
García-Recio et al (2015) The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation. PLoS One 10 e0129661 PMID: 26114632
Li et al (2013) Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells. Am J Physiol Regul Integr Comp Physiol 11 294 PMID: 23345604
Gupta et al (2007) Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol 375 29 PMID: 17295025
Nassini et al (2012) Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation. Oncotarget 7 e42454 PMID: 22905134
Sloniecka et al (2016) Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8. Mol Pharmacol 89 215 PMID: 26646648
Nassini et al (2010) Acetaminophen, via its reactive metabolite N-acetyl-p-benzo-quinoneimine and transient receptor potential ankyrin-1 stimulation, causes neurogenic inflammation in the airways and other tissues in rodents. FASEB J 24 4904 PMID: 20720158
Bang et al (2004) Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage. Br J Sports Med 308 1174 PMID: 14617692
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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.