塩酸レボカバスチン

関: levocabastine

WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/26 23:19:17」(JST)

wiki en

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]

The pharmaceutical drug Bilina is a combination of Levocabastine, Benzalkonium chloride, and other components and is typically used in a 0.5 mg/ml suspension as eye-drops, dispensed in 4ml bottles for the treatment of allergic conjunctivitis or similar allergic ocular conditions.^[10]

References

^ "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.
^ "Levocabastine ophthalmic". http://www.vademecum.es/principios-activos-levocabastina+oftalmica-s01gx02. Missing or empty |url= (help); |access-date= requires |url= (help)

External links

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.

This drug article relating to the respiratory system is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
2. 過敏性腸症候群に対するアロセトロン塩酸塩（Lotronex） alosetron hydrochloride lotronex for irritable bowel syndrome
3. クリンダマイシン：概要 clindamycin an overview
4. アレルギー性結膜炎：マネージメント allergic conjunctivitis management
5. 変形性膝関節症のマネージメント management of knee osteoarthritis

English Journal

The Administration of Levocabastine, a NTS2 Receptor Antagonist, Modifies Na(+), K(+)-ATPase Properties.

Gutnisky A1, López Ordieres MG1,2, Rodríguez de Lores Arnaiz G3.
Neurochemical research.Neurochem Res.2016 Jun;41(6):1274-80. doi: 10.1007/s11064-015-1823-7. Epub 2016 Jan 7.
Neurotensin behaves as a neuromodulator or as a neurotransmitter interacting with NTS1 and NTS2 receptors. Neurotensin in vitro inhibits synaptosomal membrane Na(+), K(+)-ATPase activity. This effect is prevented by administration of SR 48692 (antagonist for NTS1 receptor). The administration of lev
PMID 26738992

Synthesis and binding characteristics of [(3)H]neuromedin N, a NTS2 receptor ligand.

Tóth F1, Mallareddy JR1, Tourwé D2, Lipkowski AW3, Bujalska-Zadrozny M4, Benyhe S1, Ballet S2, Tóth G1, Kleczkowska P5.
Neuropeptides.Neuropeptides.2016 Jun;57:15-20. doi: 10.1016/j.npep.2015.12.004. Epub 2015 Dec 8.
Neurotensin (NT) and its analog neuromedin N (NN) are formed by the processing of a common precursor in mammalian brain tissue and intestines. The biological effects mediated by NT and NN (e.g. analgesia, hypothermia) result from the interaction with G protein-coupled receptors. The goal of this stu
PMID 26707235

Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.

Allen A1, Murdoch RD1, Bareille P1, Burns O2, Hughes S1, Gupta A3, Miller SR1.
Clinical pharmacology in drug development.Clin Pharmacol Drug Dev.2016 May;5(3):225-31. doi: 10.1002/cpdd.218. Epub 2015 Dec 4.
PURPOSE: The purpose of this study was to investigate potential systemic pharmacokinetic interactions between intranasal fluticasone furoate (FF) and levocabastine (LEVO) when delivered simultaneously via a metered atomizing spray pump.METHODS: This was a randomized, open-label, crossover study. Hea
PMID 27163502

Japanese Journal

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

香川陽人,小野利恵,矢野春奈 [他],亀井千晃
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

高村悦子,榎本雅夫,中川やよい [他]
アレルギ-・免疫 15(3), 374-383, 2008-03
NAID 40015869161

Effect of Antihistamine Eye Drops on the Conjunctival Provocation Test with Japanese Cedar Pollen Allergen

DAKE Yoshihiro,ENOMOTO Tadao,CHENG Lei,ENOMOTO Keisuke,SHIBANO Akira,IKEDA Hiroki,YODA Shigetoshi,YAJIN Shinji,SAKOTA Takema,YAMANISHI Emi
Allergology international : official journal of the Japanese Society of Allergology 55(4), 373-378, 2006-12-01
NAID 10018643080

「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; category	AU: B3; US: C (Risk not ruled out); ;
Legal status	℞ (Prescription only);
Routes of; administration	Ophthalmic, intranasal
Pharmacokinetic data
Biological half-life	3
Identifiers
CAS Number	79516-68-0
ATC code	R01AC02 S01GX02
PubChem	CID: 54385
IUPHAR/BPS	1586
DrugBank	DB01106
ChemSpider	16736421
UNII	H68BP06S81
KEGG	D08117
ChEMBL	CHEMBL1201312
Chemical data
Formula	C26H29FN2O2
Molecular 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 ;
(what is this?) (verify)

　　[★]

英: levocabastine
化: 塩酸レボカバスチン levocabastine hydrochloride
商: リボスチン
関: 眼科用剤

抗アレルギー薬

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[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.

[pmid3022160-3] 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.

[pmid2888670-4] 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.

[pmid8647296-5] 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.

[pmid8795617-6] 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.

[pmid16148226-7] 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.

[pmid17074405-8] 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.

[pmid17697051-9] 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.

[10] "Levocabastine ophthalmic". http://www.vademecum.es/principios-activos-levocabastina+oftalmica-s01gx02. Missing or empty |url= (help); |access-date= requires |url= (help)

匿名

検索

案内

案内

levocabastine hydrochloride