1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Cytoskeleton
  2. Histamine Receptor Neurotensin Receptor Integrin
  3. 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).

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Levocabastine Chemical Structure

Levocabastine Chemical Structure

CAS No. : 79516-68-0

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Description

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].

IC50 & Target[1][2][3]

H1 Receptor

 

α4β1

 

NTR2

17 nM (Ki)

In Vitro

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].

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

In Vivo

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].

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

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.
Clinical Trial
Molecular Weight

420.52

Formula

C26H29FN2O2

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

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

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  • 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.

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Levocabastine
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