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Levocabastine

Cat. No. M30621
Levocabastine Structure
Synonym:

R 50547

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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 420.52
Formula C26H29FN2O2
CAS Number 79516-68-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Levocabastine

[2] S Noble, et al. Drugs. Levocabastine. An update of its pharmacology, clinical efficacy and tolerability in the topical treatment of allergic rhinitis and conjunctivitis

[3] K L Dechant, et al. Drugs. Levocabastine. A review of its pharmacological properties and therapeutic potential as a topical antihistamine in allergic rhinitis and conjunctivitis

[4] M M Janssens, et al. Clin Exp Allergy. Levocabastine: an effective topical treatment of allergic rhinoconjunctivitis

[5] M M Janssens. Rhinol Suppl. Levocabastine: a new topical approach for the treatment of paediatric allergic rhinoconjunctivitis

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