Levocabastine

Levocabastine
Clinical data
Trade names Livostin
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration		 Ophthalmic, intranasal[1]
ATC code R01AC02 (WHO) S01GX02 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 79516-68-0 YesY
PubChem (CID) 54385
IUPHAR/BPS 1586
DrugBank DB01106 YesY
ChemSpider 16736421 YesY
UNII H68BP06S81 YesY
KEGG D08117 YesY
ChEMBL CHEMBL1201312 N
Chemical and physical data
Formula C26H29FN2O2
Molar mass 420.519 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Levocabastine (trade name Livostin) is a selective second-generation H1 receptor antagonists 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 (October 1985). "A Double-blind Evaluation of Topical Levocabastine, a New Specific H1 Antagonist in Patients with Allergic Conjunctivitis". Allergy. 40 (7): 491–6. doi:10.1111/j.1398-9995.1985.tb00255.x. PMID 2866725.
  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. doi:10.1007/BF00500016. PMID 3022160.
  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. doi:10.1016/0014-2999(87)90285-8. PMID 2888670.
  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. doi:10.1016/0014-5793(96)00397-3. PMID 8647296.
  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. PMID 8795617.
  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. doi:10.1523/JNEUROSCI.0810-05.2005. PMID 16148226.
  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. doi:10.1016/j.bbr.2006.09.016. PMID 17074405.
  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. doi:10.1111/j.1471-4159.2007.04805.x. PMID 17697051.
  10. ↑ "Levocabastine ophthalmic". http://www.vademecum.es/principios-activos-levocabastina+oftalmica-s01gx02. External link in |website= (help);


  1. ↑ "LIVOSTIN (levocabastine hydrochloride) Ophthalmic Suspension). Full Prescribing Information". DailyMed. Retrieved 4 January 2016.
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