A histamine H1 receptor antagonist
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Levocabastine (hydrochloride)

Item No. 21014

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S,4R)-1-[cis-4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid, monohydrochloride
CAS Number
79547-78-7
Molecular Formula
C26H29FN2O2 • HCl
Formula Weight
457.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): 0.33 mg/ml
λmax
261 nm
SMILES
FC(C=C1)=CC=C1[C@@](CC2)(C#N)CC[C@@H]2N(C[C@H]3C)CC[C@]3(C(O)=O)C4=CC=CC=C4.Cl
InChi Code
InChI=1S/C26H29FN2O2.ClH/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20;/h2-10,19,23H,11-17H2,1H3,(H,30,31);1H/t19-,23-,25?,26-;/m1./s1
InChi Key
OICFWWJHIMKBCD-QBRRRAQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    Levocabastine is a histamine H1 receptor antagonist (Ki = 62.5 nM).1 It is selective for histamine H1 over H2 and H3 receptors (Kis = 23.5 and 1.94 µM, respectively). Levocabastine also binds to the rat neurotensin-2 receptor (IC50 = 10 nM).2 Ocular application of levocabastine (0.025%) alone or in combination with pemirolast (Item No. 17889) reduces the severity of ovalbumin-induced conjunctivitis in ovalbumin-sensitized rats.3 Formulations containing levocabastine have been used in the treatment of seasonal allergic conjunctivitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sharif, N.A., Xu, S.X., and Yanni, J.M. Olopatadine (AL-4943A): Ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis. J. Ocul. Pharmacol. Ther. 12(4), 401-407 (1996).

    2. Chalon, P., Vita, N., Kaghad, M., et al. Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 386(2-3), 91-94 (1996).

    3. Minami, K., Hossen, M.A., and Kamei, C. Increasing effect by simultaneous use of levocabastine and pemirolast on experimental allergic conjunctivitis in rats. Biol. Pharm. Bull. 28(3), 473-476 (2005).