L3042

Sigma-Aldrich

Levocabastine hydrochloride

≥99% (HPLC), solid

Synonym(s):
[3S-[1(cis),3α,4β]]-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid, Levophta, Levostin, R50547
Empirical Formula (Hill Notation):
C26H29N2O2F·HCl
CAS Number:
Molecular Weight:
456.98
MDL number:
PubChem Substance ID:

Quality Level

assay

≥99% (HPLC)

form

solid

color

white

solubility

DMSO: soluble ~10 mg/mL

originator

Johnson & Johnson

SMILES string

Cl[H].C[C@@H]1CN(CC[C@]1(C(O)=O)c2ccccc2)[C@@H]3CC[C@@](CC3)(C#N)c4ccc(F)cc4

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-VALQNVSPSA-N

Gene Information

human ... HRH1(3269)

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Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

Non-peptide histamine H1 receptor antagonist; neurotensin NTS2 receptor ligand.

Features and Benefits

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the Neurotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

hazcat

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

storage_class_code

11 - Combustible Solids

WGK Germany

WGK 3

Personal Protective Equipment

dust mask type N95 (US),Eyeshields,Gloves

Certificate of Analysis

Certificate of Origin

Ahmed R Qasem et al.
Biochemical pharmacology, 76(6), 751-762 (2008-08-06)
Levocabastine is an antiallergic drug acting as a histamine H1-receptor antagonist. In allergic conjunctivitis (AC), it may also antagonize up-regulation of the intercellular adhesion molecule-1 (ICAM-1) expressed on epithelial conjunctival cells. However, little is known about its effects on eosinophils...
Srdjan Ante Anzic et al.
European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery, 264(11), 1309-1314 (2007-07-10)
Patients with allergic rhinitis demonstrate hyperreactive response in distilled water nasal provocation, shown by significant increase in nasal airway resistance (NAR). Antihistamines, including topical antihistamine, levocabastine, reduce response in non-specific nasal provocation tests. Furosemide is a diuretic which reduces hyperreactivity...
Bernd Lange et al.
Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology, 95(3), 272-282 (2005-10-05)
Current guidelines recommend intranasal glucocorticosteroids as first-line therapy for seasonal allergic rhinitis. To compare the efficacy, cost-effectiveness, and tolerability of the topical glucocorticosteroid mometasone furoate, the topical antihistamine levocabastine hydrochloride, and the cromone disodium cromoglycate in seasonal allergic rhinitis. This...
M Boules et al.
Brain research, 1294, 22-28 (2009-08-05)
Neurotensin (NT) is a neuropeptide with antinociceptive effects that are mediated through NT receptors, of which there are three known subtypes (NTS1, NTS2, and NTS3). Morphine is a mu-opioid receptor agonist commonly used for pain treatment but is associated with...
J M Botto et al.
Neuroscience letters, 223(3), 193-196 (1997-02-28)
The effect of the drug SR 48692 on the Ca(2+)-activated Cl- current induced by neurotensin on Xenopus oocytes injected with cRNAs encoding rodent high and low affinity neurotensin receptors, was examined. In this receptor expression system, SR 48692 failed to...

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