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Levocabastine
Systematic (IUPAC) name
(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Identifiers
CAS number 79516-68-0
ATC code R01AC02 S01GX02
PubChem 54385
DrugBank APRD01069
Chemical data
Formula C 26H29FN2O2  
Mol. mass 420.519 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 3
Excretion  ?
Therapeutic considerations
Pregnancy cat. B3(AU) C(US)
Legal status Prescription only
Routes Ophthalmic, intranasal[1]
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Levocabastine is a selective second-generation H1-receptor antagonist which was discovered at Janssen Pharmaceutica in 1979. It is used for allergic conjunctivitis.[1]

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.[2][3] This has made it a useful tool for the study of this receptor.[4][5][6][7][8]

References

  1. ^ 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.
  2. ^ 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. PMID 3022160.  
  3. ^ 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. PMID 2888670.  
  4. ^ 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. PMID 8647296. http://linkinghub.elsevier.com/retrieve/pii/0014-5793(96)00397-3.  
  5. ^ 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". The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 16 (18): 5613–20. PMID 8795617. http://www.jneurosci.org/cgi/pmidlookup?view=long&pmid=8795617.  
  6. ^ Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A (September 2005). "Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors". The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 25 (36): 8188–96. doi:10.1523/JNEUROSCI.0810-05.2005. PMID 16148226.  
  7. ^ 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.  
  8. ^ 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.  
  1. ^  "RxMed: Pharmaceutical Information - LIVOSTIN NASAL SPRAY". http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20L)/LIVOSTIN%20NASAL%20SPRAY.html. Retrieved 13 November 2005.  







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