Molecular structure of L-732,138, CAS Number: 148451-96-1
L-732,138 (CAS 148451-96-1)
Alternate Names:
3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan
Application:
L-732,138 is a selective competitive antagonist of the tachykinin NK1 receptors
CAS Number:
148451-96-1
Purity:
98%
Molecular Weight:
472.39
Molecular Formula:
C22H18F6N2O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
L-732,138 is a selective nonpeptide tachykinin NK-1R (NK1) antagonist with 1000 fold more potency towards the NK-1R receptor over NK-2R (NK2) and NK-3R (NK3) receptors with an IC50= 2.3 nM. In addition, this compound shows a 200 fold selectivity towards human NK-1R receptors compared to rat NK-1R receptors. Studies suggest that L-732,138 reduces H3 induced skin vascular permeability. L-732,138 may act to competitively inhibit the binding of [125I]L-703,606 to the NK-1R receptor. Furthermore, it is known that if histidine 265 or histidine 197 are replaced with alanine on NK-1R receptors the affinity of L-732,138 is reduced.
L-732,138 (CAS 148451-96-1) References
- Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. | Cahill, CM. and Coderre, TJ. 2002. Pain. 95: 277-285. PMID: 11839427
- Involvement of spinal neurokinin-1 receptors in the maintenance but not induction of carrageenan-induced thermal hyperalgesia in the rat. | Gao, YJ., et al. 2003. Brain Res Bull. 61: 587-93. PMID: 14519455
- Neurokinin-1 receptors located in human retinoblastoma cell lines: antitumor action of its antagonist, L-732,138. | Muñoz, M., et al. 2007. Invest Ophthalmol Vis Sci. 48: 2775-81. PMID: 17525212
- Substance P depolarizes striatal projection neurons and facilitates their glutamatergic inputs. | Blomeley, C. and Bracci, E. 2008. J Physiol. 586: 2143-55. PMID: 18308827
- Substance P mediates excitatory interactions between striatal projection neurons. | Blomeley, CP., et al. 2009. J Neurosci. 29: 4953-63. PMID: 19369564
- Tachykinin NK₁ receptor antagonist co-administration attenuates opioid withdrawal-mediated spinal microglia and astrocyte activation. | Tumati, S., et al. 2012. Eur J Pharmacol. 684: 64-70. PMID: 22724132
- Role of tachykinins and neurokinin receptor subtypes in the regulation of motility of the forestomach and abomasum in conscious sheep. | Oh-ishi, T., et al. 2013. Neuropeptides. 47: 9-18. PMID: 22938860
- The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. | Muñoz, M., et al. 2010. Cancers (Basel). 2: 611-23. PMID: 24281084
- The NK-1 receptor antagonist L-732,138 induces apoptosis in human gastrointestinal cancer cell lines. | Muñoz, M., et al. 2017. Pharmacol Rep. 69: 696-701. PMID: 28550801
- Pharmacological blockade of neurokinin1 receptor restricts morphine-induced tolerance and hyperalgesia in the rat. | Rahban, M., et al. 2022. Scand J Pain. 22: 193-203. PMID: 34525274
- Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. | Cascieri, MA., et al. 1994. J Biol Chem. 269: 6587-91. PMID: 7509807
- Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. | MacLeod, AM., et al. 1994. J Med Chem. 37: 1269-74. PMID: 7513763
- N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists. | MacLeod, AM., et al. 1993. J Med Chem. 36: 2044-5. PMID: 8393115
Inhibitor of:
NK-1R.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
L-732,138, 10 mg | sc-203437 | 10 mg | $146.00 | |||
L-732,138, 50 mg | sc-203437A | 50 mg | $466.00 |