Catalog Number: 4012
Chemical Name: 1-[2-[(3S)-3-(3,4-Dichlorophenyl)-1-[2-[3-(1-methylethoxy)phenyl]acetyl]-3-piperidinyl]ethyl]-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride
Biological Activity
Potent NK1 receptor antagonist (Ki = 0.74 nM. IC50 = 1.6 nM). Inhibits substance P-invoked calcium mobilization and outward current (IC50 = 1.3 nM); blocks NK1-mediated nitric oxide-dependent vasodilation in vivo.
Technical Data
  • M.Wt:
    656.12
  • Formula:
    C37H45Cl3N2O2
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >97%
  • Storage:
    Store at -20°C
  • CAS No:
    153050-21-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Inhibition by SR140333 of NK1 tachykinin receptor-evoked, nitric oxide-dependent vasodilation in the hamster cheek pouch microvasculature in vivo.
    Hall and Brain
    Br.J.Pharmacol., 1994;113:522
  2. Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of Caj
    Nieuwmeyer et al.
    J.Pharmacol.Exp.Ther., 2006;317:439
  3. SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line.
    Oury-Donat et al.
    J.Neurochem., 1994;62:1399
  4. In vitro and in vivo biological activities of SR140333, a novel non-peptide tachykinin NK1 receptor antagonist.
    Emonds-Alt et al.
    Eur.J.Pharmacol., 1993;250:403

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