Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Levocabastine: Difference between pages

{{Short description|Chemical compound}}

| Watchedfields = changed

| verifiedrevid = 462090822

| image = Levocabastine.svg

| width = 260

| tradename = Livostin

| legal_US = Rx-only

| legal_US_comment = <ref>{{cite web|title=Livostin - levocabastine hydrochloride suspension |url=http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=420b3f66-87f0-47d8-947c-541e84eb594a| work = DailyMed | publisher = U.S. National Library of Medicine |access-date=4 January 2016}}</ref>

| routes_of_administration = Ophthalmic, intranasal<ref>{{cite web | url = http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20L)/LIVOSTIN%20NASAL%20SPRAY.html | work = RxMed: Pharmaceutical Information | title = Livostin Nasal Spray | access-date = 13 November 2005}}</ref>

| ATC_prefix = R01

| ATC_suffix = AC02

| ATC_supplemental = {{ATC|S01|GX02}}

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| ChEMBL = 1201312

<!--Chemical data-->

| IUPAC_name = (3''S'',4''R'')-1-[''cis''-4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid

| C=26 | H=29 | F=1 | N=2 | O=2

'''Levocabastine''' (trade name '''Livostin''' or Livocab, depending on the region) is a selective second-generation [[H1 antagonist|H₁ receptor antagonist]] which was discovered at [[Janssen Pharmaceutica]] in 1979. It is used for allergic [[conjunctivitis]].<ref>{{cite journal | vauthors = Pipkorn U, Bende M, Hedner J, Hedner T | title = A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis | journal = Allergy | volume = 40 | issue = 7 | pages = 491–496 | date = October 1985 | pmid = 2866725 | doi = 10.1111/j.1398-9995.1985.tb00255.x | s2cid = 8681108 }}</ref>

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 [[Neurotensin receptor 2|NTS₂]], and was the first drug used to characterise the different neurotensin subtypes.<ref>{{cite journal | vauthors = Schotte A, Leysen JE, Laduron PM | title = Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 333 | issue = 4 | pages = 400–405 | date = August 1986 | pmid = 3022160 | doi = 10.1007/BF00500016 | s2cid = 23692347 }}</ref><ref name="pmid2888670">{{cite journal | vauthors = Kitabgi P, Rostène W, Dussaillant M, Schotte A, Laduron PM, Vincent JP | title = Two populations of neurotensin binding sites in murine brain: discrimination by the antihistamine levocabastine reveals markedly different radioautographic distribution | journal = European Journal of Pharmacology | volume = 140 | issue = 3 | pages = 285–293 | date = August 1987 | pmid = 2888670 | doi = 10.1016/0014-2999(87)90285-8 }}</ref> This has made it a useful tool for the study of this receptor.<ref name="pmid8647296">{{cite journal | vauthors = Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D | display-authors = 6 | title = Molecular cloning of a levocabastine-sensitive neurotensin binding site | journal = FEBS Letters | volume = 386 | issue = 2–3 | pages = 91–94 | date = May 1996 | pmid = 8647296 | doi = 10.1016/0014-5793(96)00397-3 | s2cid = 5802578 | doi-access = free }}</ref><ref name="pmid8795617">{{cite journal | vauthors = Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP | title = Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain | journal = The Journal of Neuroscience | volume = 16 | issue = 18 | pages = 5613–5620 | date = September 1996 | pmid = 8795617 | pmc = 6578974 | doi = 10.1523/JNEUROSCI.16-18-05613.1996 | doi-access = free }}</ref><ref name="pmid16148226">{{cite journal | vauthors = Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A | title = Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors | journal = The Journal of Neuroscience | volume = 25 | issue = 36 | pages = 8188–8196 | date = September 2005 | pmid = 16148226 | pmc = 6725526 | doi = 10.1523/JNEUROSCI.0810-05.2005 | doi-access = free }}</ref><ref name="pmid17074405">{{cite journal | vauthors = Bredeloux P, Costentin J, Dubuc I | title = Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice | journal = Behavioural Brain Research | volume = 175 | issue = 2 | pages = 399–407 | date = December 2006 | pmid = 17074405 | doi = 10.1016/j.bbr.2006.09.016 | s2cid = 24790151 }}</ref><ref name="pmid17697051">{{cite journal | vauthors = Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, Nakazawa T, Yamamoto T, Wada K | display-authors = 6 | title = Neurotensin type 2 receptor is involved in fear memory in mice | journal = Journal of Neurochemistry | volume = 102 | issue = 5 | pages = 1669–1676 | date = September 2007 | pmid = 17697051 | doi = 10.1111/j.1471-4159.2007.04805.x | s2cid = 19774998 | doi-access = free }}</ref>

The [[pharmaceutical drug]] '''Bilina''' is a combination of Levocabastine, [[benzalkonium chloride]], and other components and is typically used in a 0.5&nbsp;mg/ml suspension as eye-drops, dispensed in 4ml bottles for the treatment of allergic [[conjunctivitis]] or similar allergic ocular conditions.<ref>{{cite web|title=Levocabastine ophthalmic|website=vademecum.es |url=http://www.vademecum.es/principios-activos-levocabastina+oftalmica-s01gx02|access-date=11 September 2014}}</ref>

== References ==

{{reflist}}

== External links ==

* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/rn/79516-68-0 | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Levocabastine }}

* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/levocabastine%20hydrochloride | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Levocabastine hydrochloride }}

{{Histaminergics}}

{{Nasal preparations}}

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[[Category:Belgian inventions]]

[[Category:H1 receptor antagonists]]

[[Category:Janssen Pharmaceutica]]

[[Category:Nitriles]]

[[Category:Fluoroarenes]]

[[Category:4-Phenylpiperidines]]

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