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Levocabastine

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Title: Levocabastine  
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Subject: Neurotensin receptor, Janssen Pharmaceutica, H1 antagonist, Corbadrine, Nedocromil
Collection: Belgian Inventions, H1 Receptor Antagonists, Janssen Pharmaceutica, Nitriles, Organofluorides, Piperidines
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Levocabastine

Levocabastine
Systematic (IUPAC) name
(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Clinical data
AHFS/Drugs.com
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Legal status
  • (Prescription only)
Routes of
administration
Ophthalmic, intranasal[1]
Pharmacokinetic data
Biological half-life 3
Identifiers
CAS Registry Number  Y
ATC code R01 S01
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEMBL  N
Chemical data
Formula C26H29FN2O2
Molecular mass 420.519 g/mol
 N   

Levocabastine is a selective second-generation H1-receptor antagonist which was discovered at Janssen Pharmaceutica in 1979. It is used for allergic conjunctivitis.[2]

As well as acting as an antihistamine, levocabastine has also subsequently been found to act as a potent and selective antagonist for the neurotensin receptor NTS2, and was the first drug used to characterise the different neurotensin subtypes.[3][4] This has made it a useful tool for the study of this receptor.[5][6][7][8][9]

The pharmaceutical drug Bilina is a combination of Levocabastine, Benzalkonium chloride, and other components and is typically used in a 0.5 mg/ml suspension as eye-drops, dispensed in 4ml bottles for the treatment of allergic conjunctivitis or similar allergic ocular conditions.[10]

References

  1. ^ "RxMed: Pharmaceutical Information - LIVOSTIN NASAL SPRAY". Retrieved 13 November 2005. 
  2. ^ Pipkorn U, Bende M, Hedner J, Hedner T., A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis. Allergy. 1985 Oct;40(7):491-6.
  3. ^ Schotte A, Leysen JE, Laduron PM (August 1986). "Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology 333 (4): 400–5.  
  4. ^ Kitabgi P, Rostène W, Dussaillant M, Schotte A, Laduron PM, Vincent JP (August 1987). "Two populations of neurotensin binding sites in murine brain: discrimination by the antihistamine levocabastine reveals markedly different radioautographic distribution". European Journal of Pharmacology 140 (3): 285–93.  
  5. ^ Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D (May 1996). "Molecular cloning of a levocabastine-sensitive neurotensin binding site". FEBS Letters 386 (2-3): 91–4.  
  6. ^ Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP (September 1996). "Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain". Journal of Neuroscience 16 (18): 5613–20.  
  7. ^ Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A (September 2005). "Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors". Journal of Neuroscience 25 (36): 8188–96.  
  8. ^ Bredeloux P, Costentin J, Dubuc I (December 2006). "Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice". Behavioural Brain Research 175 (2): 399–407.  
  9. ^ Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, Nakazawa T, Yamamoto T, Wada K (September 2007). "Neurotensin type 2 receptor is involved in fear memory in mice". Journal of Neurochemistry 102 (5): 1669–76.  
  10. ^ "Levocabastine ophthalmic". http://www.vademecum.es/principios-activos-levocabastina+oftalmica-s01gx02. 

External links

  • RxList (2004). "Livostin Online, Description, Chemistry, Ingredients - Levocabastine". LIVOSTIN. RxList Inc. Retrieved 9 October 2005. 
  • Novartis Pharmaceuticals (March 2002). "LIVOSTIN" (PDF). Retrieved August 20, 2006. 


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