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Levocabastine

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This is an old revision of this page, as edited by CheMoBot (talk | contribs) at 02:47, 24 October 2011 (Updating {{drugbox}} (changes to verified fields - updated 'ChEBI_Ref', 'CAS_number_Ref') per Chem/Drugbox validation (report errors or bugs)). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Revision as of 02:47, 24 October 2011 by CheMoBot (talk | contribs) (Updating {{drugbox}} (changes to verified fields - updated 'ChEBI_Ref', 'CAS_number_Ref') per Chem/Drugbox validation (report errors or bugs))(diff) ← Previous revision | Latest revision (diff) | Newer revision → (diff) Pharmaceutical compound
Levocabastine
Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy
category
  • AU: B3
Routes of
administration		Ophthalmic, intranasal
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life3
Identifiers
IUPAC name
  • (3S,4R)-1--3-methyl-4-phenylpiperidine-4-carboxylic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H29FN2O2
Molar mass420.519 g/mol g·mol
3D model (JSmol)
SMILES
  • Fc1ccc(cc1)2(CC(CC2)N3CC((C)C3)(c4ccccc4)C(O)=O)C#N
InChI
  • 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
  • Key:ZCGOMHNNNFPNMX-KYTRFIICSA-N
  (what is this?)  (verify)

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

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. This has made it a useful tool for the study of this receptor.

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 (1986). "Evidence for a displaceable non-specific neurotensin binding site in rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology. 333 (4): 400–5. doi:10.1007/BF00500016. PMID 3022160. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  4. Kitabgi P, Rostène W, Dussaillant M, Schotte A, Laduron PM, Vincent JP (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  5. Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  6. Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  7. Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  8. Bredeloux P, Costentin J, Dubuc I (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  9. Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, Nakazawa T, Yamamoto T, Wada K (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

External links

Histamine receptor modulators
H1
Agonists
Antagonists
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
Decongestants and other nasal preparations (R01)
Topical
Sympathomimetics, plain
Antiallergic agents,
excluding corticosteroids
Corticosteroids
Other nasal preparations
Combination products
Systemic use:
Sympathomimetics

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