L-733,060 hydrochloride
1 Image
Description: Potent NK1 antagonist
Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Purity: ≥99%
Biological Activity
L-733,060 hydrochloride is a 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.Technical Data
M.Wt:
439.83
Formula:
C20H19F6NO.HCl
Solubility:
Soluble to 50 mM in water with gentle warming
Purity:
≥99%
Storage:
Store at RT
CAS No:
148687-76-7
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.
Additional Information
Licensing Caveats:
Sold with the permission of Merck, Sharpe and Dohme Ltd.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Neurokinin-1 receptor antagonism improves postoperative neurocognitive disorder in mice.
Li Z, Luo T, Ning X, Xiong C, Wu A
Neurosci Lett, 0;687(0):189-195. -
Tachykinin NK1 receptor antagonist L-733,060 and substance P deletion exert neuroprotection through inhibiting oxidative stress and cell death after traumatic brain injury in mice
Q Li, X Wu, Y Yang, Y Zhang, F He, X Xu, Z Zhang, L Tao, C Luo
Int. J. Biochem. Cell Biol., 2018;0(0):. -
Trigeminal-rostral ventromedial medulla circuitry is involved in orofacial hyperalgesia contralateral to tissue injury.
Mol Pain, 2012;8(0):78. -
Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer.
Garcia-Recio et al.
Cancer Res., 2013;73:6424 -
Distinct mechanism for antidepressant blockade of central substance P receptors.
Kramer et al.
Science, 1998;281:1640 -
L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays.
Seabrook et al.
Eur.J.Pharmacol., 1996;317:129 -
The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists.
Varty et al.
Neuropsychopharmacology, 2002;27:371
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Citations for L-733,060 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for L-733,060 hydrochloride include:
15 Citations: Showing 1 - 10
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Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages.
Authors: Muschter Et al.
Int J Mol Sci 2019;20
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The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1.
Authors: Fong Et al.
PLoS One 2017;12:e0174101
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Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla.
Authors: Khasabov Et al.
J Neurophysiol 2017;118:2727
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Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8.
Authors: Sloniecka Et al.
Mol Pharmacol 2016;89:215
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A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer.
Authors: D'Amato Et al.
Cancer Res 2015;75:4651
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The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation.
Authors: García-Recio Et al.
PLoS One 2015;10:e0129661
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Substance P reduces TNF-α-induced apoptosis in human tenocytes through NK-1 receptor stimulation.
Authors: Backman Et al.
Mol Cancer Res 2014;48:1414
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TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis.
Authors: Liu Et al.
FASEB J 2013;27:3549
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Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells.
Authors: Li Et al.
Am J Physiol Regul Integr Comp Physiol 2013;11:294
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Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation.
Authors: Nassini Et al.
Oncotarget 2012;7:e42454
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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.
Authors: Nassini Et al.
FASEB J 2010;24:4904
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Sprouting of substance P-expressing primary afferent central terminals and spinal micturition reflex NK1 receptor dependence after spinal cord injury.
Authors: Zhang Et al.
Am J Physiol Regul Integr Comp Physiol 2008;295:R2084
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TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats.
Authors: Wang Et al.
PLoS One 2008;294:R1517
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Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries.
Authors: Gupta Et al.
Naunyn Schmiedebergs Arch Pharmacol 2007;375:29
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Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage.
Authors: Bang Et al.
Br J Sports Med 2004;308:1174
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