Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Biological ActivityL-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays.
Seabrook et al.
The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists.
Varty et al.
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
Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages.
Authors: Muschter Et al.
Int J Mol Sci 2019;20
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
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
Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8.
Authors: Sloniecka Et al.
Mol Pharmacol 2016;89:215
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
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
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
TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis.
Authors: Liu Et al.
FASEB J 2013;27:3549
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
Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation.
Authors: Nassini Et al.
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
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
TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats.
Authors: Wang Et al.
PLoS One 2008;294:R1517
Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries.
Authors: Gupta Et al.
Naunyn Schmiedebergs Arch Pharmacol 2007;375:29
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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