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company name :
Tocris Bioscience
product type :
chemical
product name :
1145/10
catalog :
1145/10
quantity :
10 mg (also 50 mg)
price :
308 USD
more info or order :
citations: 19
Reference
Muschter D, Beiderbeck A, Späth T, Kirschneck C, Schröder A, Grassel S. Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages. Int J Mol Sci. 2019;20: pubmed publisher
Li Q, Wu X, Yang Y, Zhang Y, He F, Xu X, et al. 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. Int J Biochem Cell Biol. 2019;107:154-165 pubmed publisher
Li Z, Luo T, Ning X, Xiong C, Wu A. Neurokinin-1 receptor antagonism improves postoperative neurocognitive disorder in mice. Neurosci Lett. 2018;687:189-195 pubmed publisher
Khasabov S, Malecha P, Noack J, Tabakov J, Giesler G, Simone D. Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla. J Neurophysiol. 2017;118:2727-2744 pubmed publisher
Fong G, Backman L, Alfredson H, Scott A, Danielson P. The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1. PLoS ONE. 2017;12:e0174101 pubmed publisher
Słoniecka M, Le Roux S, Zhou Q, Danielson P. Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8. Mol Pharmacol. 2016;89:215-25 pubmed publisher
D Amato N, Rogers T, Gordon M, Greene L, Cochrane D, Spoelstra N, et al. A TDO2-AhR signaling axis facilitates anoikis resistance and metastasis in triple-negative breast cancer. Cancer Res. 2015;75:4651-64 pubmed publisher
García Recio S, Pastor Arroyo E, Marín Aguilera M, Almendro V, Gascón P. The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation. PLoS ONE. 2015;10:e0129661 pubmed publisher
Backman L, Eriksson D, Danielson P. Substance P reduces TNF-?-induced apoptosis in human tenocytes through NK-1 receptor stimulation. Br J Sports Med. 2014;48:1414-20 pubmed publisher
Liu B, ESCALERA J, Balakrishna S, Fan L, Caceres A, Robinson E, et al. TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J. 2013;27:3549-63 pubmed publisher
Li X, Ma G, Ma Q, Li W, Liu J, Han L, et al. Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells. Mol Cancer Res. 2013;11:294-302 pubmed publisher
Chai B, Guo W, Wei F, Dubner R, Ren K. Trigeminal-rostral ventromedial medulla circuitry is involved in orofacial hyperalgesia contralateral to tissue injury. Mol Pain. 2012;8:78 pubmed publisher
Nassini R, Pedretti P, Moretto N, Fusi C, Carnini C, Facchinetti F, et al. Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation. PLoS ONE. 2012;7:e42454 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Nassini R, Materazzi S, Andre E, Sartiani L, Aldini G, Trevisani M, 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. FASEB J. 2010;24:4904-16 pubmed publisher
Zhang X, Douglas K, Jin H, Eldaif B, Nassar R, Fraser M, et al. 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. 2008;295:R2084-96 pubmed publisher
Wang Y, Novotny M, Quaiserová Mocko V, Swain G, Wang D. TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. Am J Physiol Regul Integr Comp Physiol. 2008;294:R1517-23 pubmed publisher
Gupta S, Lozano Cuenca J, Villalón C, de Vries R, Garrelds I, Avezaat C, et al. Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol. 2007;375:29-38 pubmed
Bang R, Biburger M, Neuhuber W, Tiegs G. Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-alpha-mediated apoptotic liver damage. J Pharmacol Exp Ther. 2004;308:1174-80 pubmed
product information
master code :
1145
SKU :
1145/10
product name :
L-733,060 hydrochloride
unit size :
10 mg (also 50 mg)
description :
Potent NK1 antagonist
target :
NK1 Receptor Antagonists
category :
Small Molecules
purity :
99%
observed molecular weight :
439.83
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
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.
top caption :
Potent NK1 antagonist
extended description :
Potent NK1 antagonist
chemical name text :
(2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
formula :
C20H19F6NO.HCl
formula text :
C20H19F6NO.HCl
cas num :
148687-76-7
USD :
308 USD
product details :
Potent NK1 antagonist
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK