Levocabastine
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| Systematic (IUPAC) name | |
| (3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid | |
| Clinical data | |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Pregnancy cat. | B3(AU) C(US) |
| Legal status | ℞ Prescription only |
| Routes | Ophthalmic, intranasal[1] |
| Pharmacokinetic data | |
| Half-life | 3 |
| Identifiers | |
| CAS number | 79516-68-0  |
| ATC code | R01AC02 S01GX02 |
| PubChem | CID 54385 |
| IUPHAR ligand | 1586 |
| DrugBank | APRD01069 |
| ChemSpider | 16736421 |
| UNII | H68BP06S81 |
| KEGG | D08117 |
| ChEMBL | CHEMBL1201312  |
| Chemical data | |
| Formula | C26H29FN2O2 |
| Mol. mass | 420.519 g/mol |
| SMILES | eMolecules & PubChem |
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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.[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]
[edit] References
- ^ "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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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. http://linkinghub.elsevier.com/retrieve/pii/0014-5793(96)00397-3.
- ^ 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. http://www.jneurosci.org/cgi/pmidlookup?view=long&pmid=8795617.
- ^ 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.
- ^ 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.
- ^ 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.
[edit] External links
- RxList (2004). "Livostin Online, Description, Chemistry, Ingredients - Levocabastine". LIVOSTIN. RxList Inc. http://www.rxlist.com/drugs/drug-8041-Livostin+Opht.aspx?drugid=8041&drugname=Livostin+Opht. Retrieved 9 October 2005.[dead link]
- Novartis Pharmaceuticals (March 2002). "LIVOSTIN" (PDF). http://www.pharma.us.novartis.com/product/pi/pdf/livostin.pdf. Retrieved August 20, 2006.
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