Levocabastine - CAS 79516-68-0
Catalog number: 79516-68-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H29FN2O2
Molecular Weight:
420.52
COA:
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Targets:
Histamine Receptor
Description:
Levocabastine is a selective second-generation Histamine H1 receptor antagonist. It is used for Allergic conjunctivitis and Seasonal allergic rhinitis。Levocabastine is also a potent and selective antagonist for the neurotensin receptor NTS2 and it can be used to characterise the different neurotensin subtypes.
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Purity:
98%
Appearance:
Powder
Synonyms:
Levocabastine, Livostin, Bilina;(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
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Application:
Allergic conjunctivitis; Seasonal allergic rhinitis
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.23 g/cm3
InChIKey:
ZCGOMHNNNFPNMX-KYTRFIICSA-N
InChI:
1S/C26H29FN2O2/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)/t19-,23-,25-,26-/m1/s1
Canonical SMILES:
C[C@@H]1CN(CC[C@]1(C(=O)O)c2ccccc2)[C@@H]3CC[C@@](CC3)(C#N)c4ccc(F)cc4
Current Developer:
Janssen-Cilag; Kyowa Hakko Kirin; Nippon Shinyaku; Santen Pharmaceutical
1.In vitro effects of preserved and unpreserved anti-allergic drugs on human corneal epithelial cells.
Guzman-Aranguez A1, Calvo P, Ropero I, Pintor J. J Ocul Pharmacol Ther. 2014 Nov;30(9):790-8. doi: 10.1089/jop.2014.0030. Epub 2014 Aug 6.
PURPOSE: Treatment with topical eye drops for long-standing ocular diseases like allergy can induce detrimental side effects. The purpose of this study was to investigate in vitro cytotoxicity of commercially preserved and unpreserved anti-allergic eye drops on the viability and barrier function of monolayer and stratified human corneal-limbal epithelial cells.
2.The effect of topical corticosteroids, topical antihistamines, and preservatives on human ciliary beat frequency.
Jiao J1, Meng N, Zhang L. ORL J Otorhinolaryngol Relat Spec. 2014;76(3):127-36. doi: 10.1159/000363575. Epub 2014 Jun 24.
BACKGROUND: The aim of this study was to investigate the effect of the corticosteroids, the antihistamines, and the preservatives benzalkonium chloride (BKC) and potassium sorbate (PS) in intranasal medications on human nasal epithelial ciliary beat frequency (CBF).
3.Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Murdoch RD, Bareille P, Ignar D, Mark S, Miller SR, Gupta A, Salapatek AM, Patel P. Int J Clin Pharmacol Ther. 2015 Oct;53(10):811-8. doi: 10.5414/CP202389.
OBJECTIVES: To test the hypothesis that intranasal levocabastine (LEVO) may provide benefits as a oncedaily treatment in allergic rhinitis (AR), this non-inferiority study compared the effect at steady state of once- and twice-daily dosing with LEVO on allergen-induced nasal symptoms in AR patients.
4.Synthesis and binding characteristics of [3H]neuromedin N, a NTS2 receptor ligand.
Tóth F1, Mallareddy JR1, Tourwé D2, Lipkowski AW3, Bujalska-Zadrozny M4, Benyhe S1, Ballet S2, Tóth G1, Kleczkowska P5. Neuropeptides. 2015 Dec 8. pii: S0143-4179(15)00224-3. doi: 10.1016/j.npep.2015.12.004. [Epub ahead of print]
Neurotensin (NT) and its analog neuromedin N (NN) are formed by the processing of a common precursor in mammalian brain tissue and intestines. The biological effects mediated by NT and NN (e.g. analgesia, hypothermia) result from the interaction with G protein-coupled receptors. The goal of this study consisted of the synthesis and radiolabeling of NN, as well as the determination of the binding characteristics of [3H]NN and G protein activation by the cold ligand. In homologous displacement studies a weak affinity was determined for NN, with IC50 values of 454nM in rat brain and 425nM in rat spinal cord membranes. In saturation binding experiments the Kd value proved to be 264.8±30.18nM, while the Bmax value corresponded to 3.8±0.2pmol/mg protein in rat brain membranes. The specific binding of [3H]NN was saturable, interacting with a single set of homogenous binding sites. In sodium sensitivity experiments, a very weak inhibitory effect of Na+ ions was observed on the binding of [3H]NN, resulting in an IC50 of 150.
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CAS 79516-68-0 Levocabastine

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