Levokabastin

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Levokabastin
(IUPAC) ime
(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Klinički podaci
Identifikatori
CAS broj 79516-68-0
ATC kod R01AC02 S01GX02
PubChem[1][2] 54385
DrugBank APRD01069
ChemSpider[3] 16736421
UNII H68BP06S81 YesY
KEGG[4] D08117 YesY
ChEMBL[5] CHEMBL1201312 YesY
Hemijski podaci
Formula C26H29FN2O2 
Mol. masa 420.519 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije 3
Farmakoinformacioni podaci
Trudnoća B3(AU) C(US)
Pravni status Prescription only
Način primene Oftalmično, intranazalno[6]

Levokabastin je selektivni antagonist H1 receptora druge generacije koji je razvila kompanija Jansen Farmaceutikal 1979. On se koristi za lečenje alergijskog konjunktivitisa.[7]

Pored antihistaminskog dejstva, levokabastin takođe deluje kao potentan i selektivan antagonist neurotenzinskog receptora NTS2, i bio je prvi lek koji je korišten za karakterisanje raznih neurotenzinskih podtipova.[8][9][10][11][12][13][14]

Literatura[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Joanne Wixon, Douglas Kell (2000). "Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG". Yeast 17 (1): 48–55. doi:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. "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. pristupljeno 13 November 2005. 
  7. 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.
  8. 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. doi:10.1007/BF00500016. 
  9. 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. doi:10.1016/0014-2999(87)90285-8. 
  10. 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. doi:10.1016/0014-5793(96)00397-3. 
  11. 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. 
  12. 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. PMID 16148226. doi:10.1523/JNEUROSCI.0810-05.2005. 
  13. 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. PMID 17074405. doi:10.1016/j.bbr.2006.09.016. 
  14. 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. PMID 17697051. doi:10.1111/j.1471-4159.2007.04805.x. 

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