Bepotastine Besilate - CAS 190786-44-8
Catalog number: B0084-061917
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H31ClN2O6S
Molecular Weight:
547.063
COA:
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Targets:
Histamine Receptor
Description:
Bepotastine is a histamine H1 receptor antagonist. Bepotastine has been approved in Japan for the treatment of allergic rhinitis and uriticaria/puritus.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-061917 500 mg $248 In stock
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Brife Description:
Histamine H1 receptor antagonist
Purity:
>98%
Related CAS:
125602-71-3 (free base)
Synonyms:
Bepotastine besylate; Bepreve; Betotastine besilate; Talion; 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid, monobenzenesulfonate
MSDS:
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InChIKey:
UDGHXQPQKQPSBB-BOXHHOBZSA-N
InChI:
InChI=1S/C21H25ClN2O3.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26);1-5H,(H,7,8,9)/t21-;/m0./s1
Canonical SMILES:
C1CN(CCC1OC(C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O
1.Comparative efficacy and bioequivalence of novel h1-antihistamine bepotastine salts (nicotinate and salicylate).
Lim DS1, Youn YS, Kwack SJ, Kwak HM, Lim SK, Kim JY, Um YM, Lee JD, Hyeon JH, Kim YJ, Kim HS, Lee BM. J Toxicol Environ Health A. 2014;77(22-24):1451-66. doi: 10.1080/15287394.2014.955833.
Bepotastine salts (nicotinate and salicylate) were investigated for their physicochemical properties to develop novel salt forms of bepotastine, bioequivalent to the bepotastine besilate-loaded tablet (Talion). These bepotastine salts of either nicotinate- or salicylate-loaded tablets were prepared by conventional wet granulation method, and dissolution profiles and pharmacokinetics in beagle dogs were compared to those of Talion. A novel bepotastine nicotinate has a higher solubility at varying pH levels (1.2, 4, or 6.8) than salicylate-loaded or besilate-loaded salt. In addition, those bepostastine salt forms (nicotinate and salicylate) are stable in heat, light, and water. Further, the novel nicotinate- and salicylate-loaded tablets showed similar dissolution rates to Talion in several selected dissolution media and were bioequivalent to Talion in beagle dogs in terms of area under the concentration-time curve (AUC) and maximum observed concentration (Cmax).
2.Bepotastine besilate for the treatment of pruritus.
Bielory L1, Duttachoudhury S, McMunn A. Expert Opin Pharmacother. 2013 Dec;14(18):2553-69. doi: 10.1517/14656566.2013.849242. Epub 2013 Nov 5.
INTRODUCTION: Bepotastine besilate 1.5% is a newly approved second-generation topical antihistamine indicated for the pruritus associated with allergic conjunctivitis. In Japan, the oral formulation is approved to manage pruritus associated with allergic rhinitis and urticaria.
3.Treatment of allergic conjunctivitis with bepotastine besilate ophthalmic solution 1.5%.
Bergmann MT1, Williams JI2, Gomes PJ3. Clin Ophthalmol. 2014 Aug 13;8:1495-505. doi: 10.2147/OPTH.S66637. eCollection 2014.
PURPOSE: To examine the pooled per-protocol ocular end points from two conjunctival allergen challenge (CAC) clinical trials of the dual-action antihistamine bepotastine besilate ophthalmic solution (BBOS) 1.5%.
4.Pharmacokinetic comparisons of bepotastine besilate and bepotastine salicylate in healthy subjects.
Kim KA1, Park JY. Clin Drug Investig. 2013 Dec;33(12):913-9. doi: 10.1007/s40261-013-0140-7.
BACKGROUND AND OBJECTIVE: Bepotastine is a second-generation histamine H(1) receptor antagonist that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. The aim of the present study was to compare the pharmacokinetics of two different bepotastine formulations [bepotastine besilate 10 mg (reference) and bepotastine salicylate 9.64 mg (test)], both containing 7.11 mg bepotastine base, to satisfy regulatory requirements for marketing.
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CAS 190786-44-8 Bepotastine Besilate

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