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Chemical Compound Review

Tocris-1145     (2R,3S)-3-[[3,5- bis(trifluoromethyl)phenyl...

Synonyms: CHEMBL27006, CHEBI:137245, CCG-204837, Lopac0_000752, DNC004178, ...
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Disease relevance of L 733060


High impact information on L 733060

  • RESULTS: Nanomolar concentrations of substance P increased the growth of both cell lines and micromolar concentrations of L-733,060 inhibited the growth of the two cell lines studied, with and without previous administration of substance P [1].
  • Enantioselective inhibition of the formalin paw late phase by the NK1 receptor antagonist L-733,060 in gerbils [6].
  • In contrast, the non-brain penetrant quaternary ketone NK1 receptor antagonist, L-743,310 (3 mg/kg), did not attenuate the response to formalin, indicating that the antinociceptive effect of blockade of NK1 receptors by L-733,060 in this assay is centrally-mediated [6].
  • Also, pretreatment with the specific NK-1 receptor antagonist (2S,3S)-3-([3,5-bis[trifluoromethyl)phenyl]methoxy)-2-phenylpiperidine (L-733,060) significantly inhibited the inflammatory effects of both toxin A and anandamide [7].
  • In guinea-pigs, i.c.v. infusion of the selective substance P agonist GR73632 (0.1 nmol) elicited a pronounced vocalisation response that was blocked enantioselectively by the NK(1) receptor antagonists CP-99,994 and L-733,060 (0.1-10 mg/kg) [8].

Biological context of L 733060


Anatomical context of L 733060


Associations of L 733060 with other chemical compounds

  • Similarly, vocalisations in guinea-pig pups separated from their mothers were blocked enantioselectively by the highly brain-penetrant NK(1) receptor antagonists L-733,060 and GR205171 (ID(50) 3 mg/kg), but not by the poorly brain-penetrant compounds LY303870 and CGP49823 (30 mg/kg) [8].
  • In separate experiments two different neurokinin-1 (NK-1) receptor antagonists (D-Arg(1), D-Pro(2), D-Trp(7,9), Leu(11), or L-733,060) were perfused via the microdialysis probe for one hour in awake and freely moving animals that were subsequently injected i.p. with cocaine [11].
  • In a separate experiment, infusion through the microdialysis probe of the neurokinin-1 receptor antagonist L-733,060 significantly decreased cocaine-evoked striatal dopamine overflow (approximately 50% inhibition at 30 minutes after cocaine administration) [12].
  • This loss was prevented by preexposure (30 min before the first injection of methamphetamine) of the neurokinin-1 receptor antagonist L-733,060 [13].
  • Furthermore, oral administration of the NK1 antagonists MK-869 (10 mg/kg), L-742694 (10 mg/kg), L-733060 (10 mg/kg), CP-99994 (30 mg/kg), and CP-122721 (3-30 mg/kg) reduced immobility time [14].

Gene context of L 733060

  • We infused the neurokinin-1 receptor (NK-1R) antagonist, L-733,060, into the striatum of freely moving rats via a microdialysis probe in order to assess the effects of SP on cocaine-induced DA overflow in the striatum [15].
  • L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays [16].
  • The SP-specific NK-1 receptor antagonist L-733060 did not influence fEPSP in a concentration of 1 microM [9].


  1. Antitumoral action of the neurokinin-1-receptor antagonist L-733,060 and mitogenic action of substance P on human retinoblastoma cell lines. Muñoz, M., Rosso, M., Pérez, A., Coveñas, R., Rosso, R., Zamarriego, C., Soult, J.A., Montero, I. Invest. Ophthalmol. Vis. Sci. (2005) [Pubmed]
  2. Neurokinin-1 (NK-1) receptor antagonists abrogate methamphetamine-induced striatal dopaminergic neurotoxicity in the murine brain. Yu, J., Cadet, J.L., Angulo, J.A. J. Neurochem. (2002) [Pubmed]
  3. A general approach to (5S,6R)-6-alkyl-5-benzyloxy-2-piperidinones: application to the asymmetric syntheses of neurokinin substance P receptor antagonist (-)-L-733,061 and (-)-deoxocassine. Liu, L.X., Ruan, Y.P., Guo, Z.Q., Huang, P.Q. J. Org. Chem. (2004) [Pubmed]
  4. The NK1 receptor is involved in the antitumoural action of L-733,060 and in the mitogenic action of substance P on neuroblastoma and glioma cell lines. Muñoz, M., Rosso, M., Pérez, A., Coveñas, R., Rosso, R., Zamarriego, C., Piruat, J.I. Neuropeptides (2005) [Pubmed]
  5. Antitumoural action of L-733,060 on neuroblastoma and glioma cell lines. Muñoz, M., Pérez, A., Coveñas, R., Rosso, M., Castro, E. Archives italiennes de biologie. (2004) [Pubmed]
  6. Enantioselective inhibition of the formalin paw late phase by the NK1 receptor antagonist L-733,060 in gerbils. Rupniak, N.M., Carlson, E., Boyce, S., Webb, J.K., Hill, R.G. Pain (1996) [Pubmed]
  7. Endocannabinoids induce ileitis in rats via the capsaicin receptor (VR1). McVey, D.C., Schmid, P.C., Schmid, H.H., Vigna, S.R. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  8. Pharmacological blockade or genetic deletion of substance P (NK(1)) receptors attenuates neonatal vocalisation in guinea-pigs and mice. Rupniak, N.M., Carlson, E.C., Harrison, T., Oates, B., Seward, E., Owen, S., de Felipe, C., Hunt, S., Wheeldon, A. Neuropharmacology (2000) [Pubmed]
  9. Effects of substance P and its antagonist L-733060 on long term potentiation in guinea pig hippocampal slices. Langosch, J.M., Kupferschmid, S., Heinen, M., Walden, J., Herpfer, I., Fiebich, B.L., Lieb, K. Prog. Neuropsychopharmacol. Biol. Psychiatry (2005) [Pubmed]
  10. No modulatory effect of neurokinin-1 receptor antagonists on serotonin uptake in human and rat brain synaptosomes. Lieb, K., Fiebich, B.L., Herpfer, I., Mantovani, M., Löffler, M., Feuerstein, T.J. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. (2005) [Pubmed]
  11. Neurokinin receptors modulate the neurochemical actions of cocaine. Noailles, P.A., Angulo, J.A. Ann. N. Y. Acad. Sci. (2002) [Pubmed]
  12. Substance P modulates cocaine-evoked dopamine overflow in the striatum of the rat brain. Kraft, M., Noailles, P., Angulo, J.A. Ann. N. Y. Acad. Sci. (2001) [Pubmed]
  13. Ontogeny of neurokinin-1 receptor mediation of methamphetamine neurotoxicity in the striatum of the mouse brain. Yu, J., Allison, S., Ibrahim, D., Cadet, J.L., Angulo, J.A. Ann. N. Y. Acad. Sci. (2002) [Pubmed]
  14. The antidepressant-like effects of neurokinin NK1 receptor antagonists in a gerbil tail suspension test. Varty, G.B., Cohen-Williams, M.E., Hunter, J.C. Behavioural pharmacology. (2003) [Pubmed]
  15. Substance P and cholecystokinin regulate neurochemical responses to cocaine and methamphetamine in the striatum. Loonam, T.M., Noailles, P.A., Yu, J., Zhu, J.P., Angulo, J.A. Life Sci. (2003) [Pubmed]
  16. L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Seabrook, G.R., Shepheard, S.L., Williamson, D.J., Tyrer, P., Rigby, M., Cascieri, M.A., Harrison, T., Hargreaves, R.J., Hill, R.G. Eur. J. Pharmacol. (1996) [Pubmed]
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