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L-733060

L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain[1][2][3].

Product Specifications

CAS Number

[148700-85-0]

UNSPSC

12352005

Target

Neurokinin Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Smiles

FC(C1=CC(C(F)(F)F)=CC(CO[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)=C1)(F)F

Molecular Formula

C20H19F6NO

Molecular Weight

403.36

References & Citations

[1]Langosch JM, et al. Effects of substance P and its antagonist L-733060 on long term potentiation in guinea pig hippocampal slices. Prog Neuropsychopharmacol Biol Psychiatry. 2005 Feb;29 (2) :315-9. |[2]SI-Yi Mo et al. Neuronal Activities in the Rostral Ventromedial Medulla Associated with Experimental Occlusal Interference-Induced Orofacial Hyperalgesia. J Neurosci. 2022 Jul 6;42 (27) :5314-5329. |[3]Muñoz M, et, al. Antitumoral action of the neurokinin-1 receptor antagonist L-733 060 on human melanoma cell lines. Melanoma Res. 2004 Jun;14 (3) :183-8.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

NK1R

Curated Selection

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