Levocabastine hydrochloride  (Synonyms: R 50547 hydrochloride)

Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a K_i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)^[1][2][3].

Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of ¹²⁵I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC₅₀ of 406.2μm^[3].
Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC₅₀ of 395.6 μM, and the adhesion of EoL-1 cells with an IC₅₀ of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC₅₀=443.7 μM)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness^[1].
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior^[2].
Levocabastine (500 μg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

456.98

C₂₆H₃₀ClFN₂O₂

79547-78-7

Solid

White to off-white

OC([C@@]1(C2=CC=CC=C2)[C@@H](CN([C@]3([H])CC[C@](CC3)(C4=CC=C(C=C4)F)C#N)CC1)C)=O.[H]Cl

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Folkerts G, et, al. Virus-induced airway hyperresponsiveness in the guinea-pig: possible involvement of histamine and inflammatory cells. Br J Pharmacol. 1993 Apr;108(4):1083-93.  [Content Brief]

  [2]. Yamauchi R, et, al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006 Dec;27(12):3176-82.  [Content Brief]

  [3]. Qasem AR, et, al. Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62.  [Content Brief]