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Chemical Compound Review:

Lopac-A-5330 [3,5-bis(trifluoromethyl) phenyl]methyl...

Synonyms: Tocris-0868, CHEMBL22870, A5330_SIGMA, CCG-204124, Lopac0_000028, ...

Cahill, C.M. et al., Cascieri, M.A. et al., El-Mahmoudy, A. et al., Lewis, R.T. et al.

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Disease relevance of L 732138

L-732,138 (5-200 nmol) administered i.t. prior to and for 3 consecutive days post-surgery attenuated the mechanical allodynia and cold hyperalgesia on days 4 and 8 post-surgery [1].

High impact information on L 732138

L-732,138 inhibits the binding of 125I-substance P to the cloned human NK1 receptor expressed in Chinese hamster ovary cells with an IC50 of 2.3 +/- 0.7 nM [2].
We now report the detailed characterization of the interaction of N-acetyl-L-tryptophan-3,5-bistrifluoromethyl benzyl ester (L-732,138) with the human neurokinin-1 (NK-1) receptor [2].
In this study, the non-peptide neurokinin-1 (NK-1) receptor antagonist, L-732,138 was chronically administered by intrathecal (i.t.) injection to rats with mono-neuropathy produced by sciatic nerve constriction [1].
Application of SP antagonist, L-732,138, (1 microM) markedly inhibited EJP (82.5%) and contraction (68.9%) and completely blocked excitatory responses produced by exogenous application of SP [3].

Associations of L 732138 with other chemical compounds

The 3,5-bis(trifluoromethyl)benzyl ester of N-acetyl-L-tryptophan 1 (L-732,138) has been identified previously as a potent and selective substance P receptor antagonist [4].

References

Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. Cahill, C.M., Coderre, T.J. Pain (2002) [Pubmed]
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. Cascieri, M.A., Macleod, A.M., Underwood, D., Shiao, L.L., Ber, E., Sadowski, S., Yu, H., Merchant, K.J., Swain, C.J., Strader, C.D. J. Biol. Chem. (1994) [Pubmed]
Tachykinins mediate non-adrenergic, non-cholinergic excitatory neurotransmission to the hamster ileum via NK1 and NK2 receptors. El-Mahmoudy, A., Matsuyama, H., Khalifa, M., Shimizu, Y., Takewaki, T. Life Sci. (2003) [Pubmed]
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage. Lewis, R.T., Macleod, A.M., Merchant, K.J., Kelleher, F., Sanderson, I., Herbert, R.H., Cascieri, M.A., Sadowski, S., Ball, R.G., Hoogsteen, K. J. Med. Chem. (1995) [Pubmed]

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