L-733060 (hydrochloride)

L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride 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 hydrochloride can be used for the study of chronic orofacial pain[1][2][3].

Product Specifications

CAS Number

[148687-76-7]

UNSPSC

12352005

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/l-733060-hydrochloride.html

Purity

99.9

Solubility

H2O : 22 mg/mL (warming)

Smiles

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

Molecular Formula

C20H20ClF6NO

Molecular Weight

439.82

References & Citations

[1]Seabrook GR, et, al. L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur J Pharmacol. 1996 Dec 12; 317 (1) :129-35.|[2]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.|[3]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.