L-733,060 hydrochloride

• Supplier: Tocris Bioscience
• Catalog: 0868
• Prices: $199.00, $825.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 148687-76-7
• Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidinehydrochloride
• Formula: C20H19F6NO.HCl
• Molecular Weight: 439.83
• Purity: >99 %
• Description: Potent NK 1 antagonist (K i 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.

Product References

L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i - L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i

Seabrook GR, Shepheard SL, Williamson DJ, Tyrer P, Rigby M, Cascieri MA, Harrison T, Hargreaves RJ, Hill RG. Eur J Pharmacol. 1996 Dec 12;317(1):129-35.

Distinct mechanism for antidepressant activity by blockade of central substance P - Distinct mechanism for antidepressant activity by blockade of central substance P

Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek JJ, Reines SA, Liu G, Snavely D, Wyatt-Knowles E, Hale JJ, Mills SG, MacCoss M, Swain CJ, Harrison T, Hill RG, Hefti F, Scolnick EM, Cascieri MA, Chicchi GG, Sadowski S, Williams AR, Hewson L, Smith D, Carlson EJ, Hargreaves RJ, Rupniak NM. Science. 1998 Sep 11;281(5383):1640-5.

The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin - The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin

Varty GB, Cohen-Williams ME, Morgan CA, Pylak U, Duffy RA, Lachowicz JE, Carey GJ, Coffin VL. Neuropsychopharmacology. 2002 Sep;27(3):371-9.

NK-1 receptor antagonists induce apoptosis and counteract substance P-related - NK-1 receptor antagonists induce apoptosis and counteract substance P-related

Munoz M, Rosso M, Aguilar FJ, Gonzalez-Moles MA, Redondo M, Esteban F. Invest New Drugs. 2008 Apr;26(2):111-8. Epub 2007 Sep 29.