L-733060

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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.

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L-733060 Chemical Structure

CAS No. : 148700-85-0

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Other In-stock Forms of L-733060:

L-733060 hydrochloride

Other Forms of L-733060:

L-733060 hydrochloride In-stock

1 Publications Citing Use of MCE L-733060

•Nat Commun. 2025 Mar 31;16(1):3093. [Abstract]

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NK1R NK2R NK3R

Biological Activity
Purity & Documentation
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Description

IC₅₀ & Target^[1]^[2]

NK1R

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.87 nM Compound: 1	Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells	10.1016/0960-894X(95)00009-I
CHO	IC₅₀	0.87 nM Compound: 4	Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells	[PMID: 8627597]
CHO	IC₅₀	1 nM Compound: (+/-)2 (2S, 3S)	Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells	10.1016/S0960-894X(01)80280-8
CHO	IC₅₀	1 nM Compound: 2	Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells	10.1016/0960-894X(95)00220-N
CHO	IC₅₀	1 nM Compound: 2	Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells	[PMID: 9873445]
CHO	IC₅₀	1 nM Compound: 4	Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells. Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells.	[PMID: 9804702]
CHO	IC₅₀	1 nM Compound: L-733060	Binding affinity for human NK1 receptor expressed in CHO cells Binding affinity for human NK1 receptor expressed in CHO cells	10.1016/S0960-894X(01)80585-0

Molecular Weight

403.36

Formula

C₂₀H₁₉F₆NO

CAS No.

148700-85-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

L-733060 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-733060148700-85-0L733060L 733060Neurokinin ReceptorNK receptorTachykinin receptorNK-1 receptor antagonistorofacial hyperalgesiarostral ventromedial medulladescending pain modulationchronic pain maintenanceInhibitorinhibitorinhibit

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