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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/12/09 13:36:54」(JST)

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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]

References[edit]

^ "RxMed: Pharmaceutical Information - LIVOSTIN NASAL SPRAY". 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.
^ 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.
^ 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.

External links[edit]

RxList (2004). "Livostin Online, Description, Chemistry, Ingredients - Levocabastine". LIVOSTIN. RxList Inc. Retrieved 9 October 2005. ^{[dead link]}
Novartis Pharmaceuticals (March 2002). "LIVOSTIN" (PDF). Retrieved August 20, 2006.

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1. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis

English Journal

[Safety and efficacy of a new preservative-free levocabastine ophthalmic solution (Levofree(®)) using the conjunctival provocation test.]

Allaire C, Siou-Mermet R, Bassols A.SourceBausch+Lomb, laboratoire Chauvin SA, 416, rue Samuel-Morse, CS 99535, 34961 Montpellier cedex 2, France.
Journal francais d'ophtalmologie.J Fr Ophtalmol.2012 Apr 10. [Epub ahead of print]
OBJECTIVES: To evaluate the safety and efficacy of preservative-free levocabastine 0.05 % ophthalmic solution compared to placebo (vehicle) and to preserved levocabastine 0.05 % ophthalmic suspension in the prevention of allergic conjunctivitis induced by a conjunctival provocation test.METHODS: N
PMID 22498504

Neurotensin decreases high affinity [3H]-ouabain binding to cerebral cortex membranes.

Rosin C, Ordieres MG, Arnaiz GR.SourceInstituto de Biología Celular y Neurociencias Prof. E. De Robertis, CONICET-UBA, Facultad de Medicina, Universidad de Buenos Aires, Junín 956, 1113-Buenos Aires, Argentina.
Regulatory peptides.Regul Pept.2011 Dec 10;172(1-3):35-40. Epub 2011 Sep 5.
Previous work from this laboratory showed the ability of neurotensin to inhibit synaptosomal membrane Na(+), K(+)-ATPase activity, the effect being blocked by SR 48692, a non-peptidic antagonist for high affinity neurotensin receptor (NTS1) [López Ordieres and Rodríguez de Lores Arnaiz 2000; 2001]
PMID 21896291

Japanese Journal

アレルギー性結膜炎における冷却シートの効果と涙液中ヒスタミン濃度

YAKUGAKU ZASSHI 130(7), 971-975, 2010
NAID 130000308762

ラットのアレルギー性結膜炎モデルに対するリボスチン^【○!R】点眼液およびレボカバスチン塩酸塩点眼液「わかもと」の効果の比較

あたらしい眼科 = Journal of the eye 26(9), 1257-1260, 2009-09-30
NAID 10026256320

花粉曝露室においてスギ花粉により誘発される眼アレルギー症状--塩酸レボカバスチン点眼液(リボスチン点眼液0.025%)と塩酸オロパタジン点眼液(パタノール点眼液0.1%)の臨床効果

アレルギ-・免疫 15(3), 374-383, 2008-03
NAID 40015869161

「レボカバスチン」

Levocabastine
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
Pharmacokinetic data
Half-life	3
Identifiers
CAS number	79516-68-0
ATC code	R01AC02 S01GX02
PubChem	CID 54385
IUPHAR ligand	1586
DrugBank	DB01106
ChemSpider	16736421
UNII	H68BP06S81
KEGG	D08117
ChEMBL	CHEMBL1201312
Chemical data
Formula	C26H29FN2O2
Mol. mass	420.519 g/mol
	SMILES Fc1ccc(cc1)[C@]2(CC[C@@H](CC2)N3CC[C@@]([C@H](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 ;
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