ベ・タスチン
- 関
- bepotastine besilate
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/10/20 02:42:53」(JST)
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Bepotastine
|
Systematic (IUPAC) name |
4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
|
Clinical data |
AHFS/Drugs.com |
International Drug Names |
MedlinePlus |
a610012 |
Pregnancy
category |
- US: C (Risk not ruled out)
|
Legal status |
|
Routes of
administration |
Oral, topical (eye drops) |
Pharmacokinetic data |
Bioavailability |
High (oral)
Minimal (topical) |
Protein binding |
~55% |
Excretion |
Renal (75–90%) |
Identifiers |
CAS Registry Number |
125602-71-3 N |
ATC code |
None |
PubChem |
CID: 2350 |
DrugBank |
DB04890 Y |
ChemSpider |
2260 Y |
UNII |
HYD2U48IAS Y |
KEGG |
D09705 Y |
ChEBI |
CHEBI:71204 N |
ChEMBL |
CHEMBL1201758 N |
Chemical data |
Formula |
C21H25ClN2O3 |
Molecular mass |
388.88 g/mol |
SMILES
-
Clc1ccc(cc1)C(OC2CCN(CCCC(=O)O)CC2)c3ncccc3
|
InChI
-
InChI=1S/C21H25ClN2O3/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26) Y
-
Key:YWGDOWXRIALTES-UHFFFAOYSA-N Y
|
N (what is this?) (verify) |
Bepotastine (Talion) is a 2nd-generation antihistamine.[1] It was approved in Japan for use in the treatment of allergic rhinitis and urticaria/pruritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name TALION. TALION was co-developed by Tanabe Seiyaku and Ube Industries, Ltd., who discovered bepotastine. In 2001, Tanabe Seiyaku granted Senju exclusive worldwide rights, with the exception of certain Asian countries, to develop, manufacture and market bepotastine for ophthalmic use. Senju, in turn, has granted the United States rights for the ophthalmic preparation to ISTA Pharmaceuticals, Inc., a specialty pharmaceutical company located in Irvine, CA.
References
- ^ H. Takahashi, A. Ishida-Yamamoto, H. Iizuka (September 2004). "Effects of bepotastine, cetirizine, fexofenadine, and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performance". Clinical and Experimental Dermatology 29: 526–532. doi:10.1111/j.1365-2230.2004.01618.x.
Histaminergics
|
|
Receptor
(ligands) |
H1 |
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- UR-AK49
- Antagonists: First-generation: 4-Methyldiphenhydramine
- Alimemazine
- Antazoline
- Azatadine
- Bamipine
- Benzatropine (benztropine)
- Bepotastine
- Bromazine
- Brompheniramine
- Buclizine
- Captodiame
- Carbinoxamine
- Chlorcyclizine
- Chloropyramine
- Chlorothen
- Chlorphenamine
- Chlorphenoxamine
- Cinnarizine
- Clemastine
- Clobenzepam
- Clocinizine
- Cyclizine
- Cyproheptadine
- Dacemazine
- Decloxizine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine (ethylbenztropine)
- Etymemazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Medrylamine
- Mepyramine (pyrilamine)
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- Second/third-generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Desloratadine
- Dorastine
- Ebastine
- Efletirizine
- Emedastine
- Epinastine
- Fexofenadine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Levocetirizine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Pibaxizine
- Piclopastine
- Rocastine
- Rupatadine
- Setastine
- Talastine
- Temelastine
- Terfenadine
- Vapitadine
- Zepastine
- Non-generational: Atypical antipsychotics (e.g., aripiprazole, asenapine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
- Unknown/unsorted: Belarizine
- Elbanizine
- Flotrenizine
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
|
|
H2 |
- Agonists: Amthamine
- Betazole
- Dimaprit
- Histamine
- HTMT
- Impromidine
- UR-AK49
- Antagonists: Bisfentidine
- Burimamide
- Cimetidine
- Dalcotidine
- Donetidine
- Ebrotidine
- Etintidine
- Famotidine
- Lafutidine
- Lamtidine
- Lavoltidine (loxtidine)
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine (quisultidine)
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
|
|
H3 |
- Agonists: α-Methylhistamine
- Cipralisant
- Histamine
- Imetit
- Immepip
- Immethridine
- Methimepip
- Proxyfan
- Antagonists: A-349,821
- A-423,579
- ABT-239
- ABT-652
- AZD5213
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- Enerisant
- GSK-189,254
- Impentamine
- Iodophenpropit
- Irdabisant
- JNJ-5207852
- MK-0249
- NNC 38-1049
- PF-03654746
- Pitolisant
- SCH-79687
- Thioperamide
- VUF-5681
|
|
H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- VUF-8430
- Antagonists: JNJ-7777120
- Mianserin
- Thioperamide
- Toreforant
- VUF-6002
|
|
|
Transporter
(inhibitors) |
VMATs |
TAAR1 inactive |
- Amiodarone
- APP
- AZIK
- Bietaserpine
- Deserpidine
- Dihydrotetrabenazine
- Efavirenz
- GBR-12935
- GZ-793A
- Ibogaine
- Ketanserin
- Lobeline
- Methoxytetrabenazine
- NBI-98854
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- Vanoxerine (GBR-12909)
|
|
TAAR1 active |
- Amphetamine
- Methamphetamine
- MDMA
- Phenethylamine
|
|
|
|
Enzyme
(inhibitors) |
HDC |
- Catechin
- Meciadanol
- Naringenin
- Tritoqualine
|
|
HNMT |
- Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
|
|
DAO |
|
|
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Others |
|
|
Index of the respiratory system
|
|
Description |
- Anatomy
- Physiology
- Development
|
|
Disease |
- Congenital
- Neoplasms and cancer
- Chest trauma
- Infection
- common cold
- pneumonia
- tuberculosis
- Other
- Symptoms and signs
|
|
Treatment |
- Procedures
- Drugs
- nasal
- throat
- obstructive airway diseases
- cough and cold
- histaminergics
- pulmonary arterial hypertension
- other
- Surgery
|
|
|
UpToDate Contents
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English Journal
- Effects of Bepotastine and Fexofenadine on Histamine-Induced Flare, Wheal and Itch.
- Tanizaki H, Ikoma A, Fukuoka M, Miyachi Y, Kabashima K.SourceDepartment of Dermatology, Kyoto University Graduate School of Medicine, Kyoto, Japan.
- International archives of allergy and immunology.Int Arch Allergy Immunol.2012 Jan 26;158(2):191-195. [Epub ahead of print]
- Background: Urticaria is mainly caused by mast cell-derived histamine through the histamine H(1) receptor. Antihistamines are occasionally used on demand upon a recurrence of urticaria; therefore, rapidly acting agents should be explored. The onset of action is assumed to depend on time to maximum c
- PMID 22286689
- Histamine and H1-antihistamines: celebrating a century of progress.
- Simons FE, Simons KJ.SourceDepartment of Pediatrics & Child Health and the Department of Immunology, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada. lmcniven@hsc.mb.ca
- The Journal of allergy and clinical immunology.J Allergy Clin Immunol.2011 Dec;128(6):1139-1150.e4. Epub 2011 Oct 27.
- In this review we celebrate a century of progress since the initial description of the physiologic and pathologic roles of histamine and 70 years of progress since the introduction of H(1)-antihistamines for clinical use. We discuss histamine and clinically relevant information about the molecular m
- PMID 22035879
Japanese Journal
- 治療 ベポタスチンベシル酸塩口腔内崩壊錠の服薬コンプライアンスに与える'医師による味に関する事前説明'の影響
- そう痒性皮膚疾患におけるベシル酸ベポタスチンの臨床的効果に関するアンケート調査
- 大森 睦美,竹内 聡,田代 あかり [他],中原 剛志,三苫 千景,寺尾 浩,浦田 保志,吉村 映里,工藤 恭子,安川 晋輔,辻田 淳,国場 尚志,増永 可奈,桑原 健太郎,市川 竜太郎,伊藤 絵里子,竹下 弘道,安川 史子,西江 温子,師井 洋一,古江 増隆
- 西日本皮膚科 = The Nishinihon journal of dermatology 72(3), 240-245, 2010-06-01
- NAID 10026929692
- ベポタスチンベシル酸塩のスギ花粉症に対する臨床効果--睡眠に関する検討
Related Links
- 1. Clin Exp Dermatol. 2004 Sep;29(5):526-32. Effects of bepotastine, cetirizine, fexofenadine, and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performance. Takahashi H, Ishida-Yamamoto A ...
- Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. ... Ordering online To place an order online, simply browse to the product you are interested in and click on the 'Add to Cart' button. To complete ...
★リンクテーブル★
[★]
- 英
- bepotastine、
- 化
- ベシル酸ベポタスチン bepotastine besilate
[★]
- 関
- bepotastine