levocabastine

Levocabastine (R 50547) 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 Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Signaling Pathways >> GPCR/G Protein >> Neurotensin Receptor

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Integrin

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

H1 Receptor

α4β1

NTR2:17 nM (Ki)

Levocabastine (0-1000 μM; HEK-293 cells) 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) 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].

Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) inhibits the virus-induced airway hyperresponsiveness[1]. Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) blocks anti-stress effect ofβ-LT on mouse behavior[2]. Levocabastine (500 µg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4[3]. Animal Model: Guinea-pig with Parainfluenza-3 (PI-3) virus[1] Dosage: 0.25 mg/kg Administration: Intraperitoneal injection; twice a day for five days Result: Suppressed the influx of broncho-alveolar cells and increased in albumin content. Animal Model: Male C57BL/6J mice (8-9 weeks old)[2] Dosage: 0.05 mg/kg; 30 mg/kg (β-LT) Administration: Intraperitoneal injection; once Result: Blocked the anxiolytic effect of β-LT and decreased the number of head-dips. Animal Model: Ovalbumin-sensitized guinea pigs[3] Dosage: 500 µg/eye Administration: drops eye, once Result: Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration.