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]. IC50 & Target:NK1 Receptor^[1] In Vitro:L-733060 (30-300 nM) inhibits the [Ca²⁺]_i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK₁ receptor-transfected CHO cells^[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells^[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC₅₀s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively^[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC₅₀s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively^[2]. In Vivo:L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats^[1].
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats^[1].