Emedastine Difumerate

  • CAT Number: R043027
  • CAS Number: 87233-62-3
  • Molecular Formula: C25H34N4O9
  • Molecular Weight: 534.566
  • Purity: ≥95%
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Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. This medication is an antihistamine, prescribed for allergic conjunctivitis. It blocks histamine/’s action, which reduces allergy symptoms. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result, this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva.

Catalog Number R043027
CAS Number 87233-62-3
Synonyms

1H-1,4-Diazepine 1H-Benzimidazole deriv. Difumerate; 1-Methyl-4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)[1,4]diazepane Difumerate;

Molecular Formula

C25H34N4O9

Purity 95%
Target Histamine H1 Receptor Antagonist
Storage -20°C
IUPAC Name (E)-but-2-enedioic acid;1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole
InChI InChI=1S/C17H26N4O.2C4H4O4/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20;2*5-3(6)1-2-4(7)8/h4-5,7-8H,3,6,9-14H2,1-2H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1+
InChIKey FWLKKPKZQYVAFR-LVEZLNDCSA-N
SMILES CCOCCN1C2=CC=CC=C2N=C1N3CCCN(CC3)C.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
Reference

</br>1: Murota H, Katayama I. Emedastine difumarate: a review of its potential</br> ameliorating effect for tissue remodeling in allergic diseases. Expert Opin</br> Pharmacother. 2009 Aug;10(11):1859-67. doi: 10.1517/14656560903078410. Review.</br> PubMed PMID: 19558341.</br>2: Tian Y, Zhang Z, Liang J, Li W, Chen Y. High-performance liquid</br> chromatography-electrospray ionization-mass spectrometric determination of</br> emedastine difumarate in human plasma and its pharmacokinetics. J Chromatogr Sci.</br> 2007 Mar;45(3):158-64. PubMed PMID: 17462131.</br>3: Pons-Guiraud A, Nekam K, Lahovsky J, Costa A, Piacentini A. Emedastine</br> difumarate versus loratadine in chronic idiopathic urticaria: a randomized,</br> double-blind, controlled European multicentre clinical trial. Eur J Dermatol.</br> 2006 Nov-Dec;16(6):649-54. PubMed PMID: 17229605.</br>4: Corrado ME, Radicioni MM, Hartwig J, Assandri A, Oldeman HG, Mion A. Clinical </br> study of the therapeutic efficacy and safety of emedastine difumarate versus</br> terfenadine in the treatment of seasonal allergic rhinitis.</br> Arzneimittelforschung. 2004;54(10):660-5. PubMed PMID: 15553105.</br>5: Brunner M, Kletter K, Assandri A, Ermanno Corrado M, Eichler HG, Müller M.</br> Pharmacokinetic and mass balance study of unlabelled and (14)C-labelled</br> emedastine difumarate in healthy volunteers. Xenobiotica. 2002 Sep;32(9):761-70. </br> PubMed PMID: 12396273.</br>6: D/’Arienzo PA, Leonardi A, Bensch G. Randomized, double-masked,</br> placebo-controlled comparison of the efficacy of emedastine difumarate 0.05%</br> ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the</br> human conjunctival allergen challenge model. Clin Ther. 2002 Mar;24(3):409-16.</br> PubMed PMID: 11952024.</br>7: Joukhadar C, Herranz U, Pernerstorfer T, Assandri A, Klein N, Schrolnberger C,</br> Lackner E, Eichler HG, Müller M. Pharmacokinetics of emedastine difumarate, a new</br> anti-histaminic agent in patients with renal impairment. Eur J Clin Pharmacol.</br> 2001 Mar;56(12):905-10. PubMed PMID: 11317479.</br>8: Okubo K, Pawankar R, Gotoh M, Yagi T. Adhesive explant culture of allergic</br> nasal mucosa: effect of emedastine difumarate, an anti-allergic drug. Jpn J</br> Pharmacol. 1999 Mar;79(3):351-7. PubMed PMID: 10230864.</br>9: Hamada T, Kawashima T, Awata N. [Selective and sensitive determination of an</br> antiallergic agent, emedastine difumarate (KG-2413), in human plasma by the</br> radioreceptor assay combined with a high-performance liquid chromatography].</br> Yakugaku Zasshi. 1989 Oct;109(10):749-54. Japanese. PubMed PMID: 2576060.</br>10: Murota H, Bae S, Hamasaki Y, Maruyama R, Katayama I. Emedastine difumarate</br> inhibits histamine-induced collagen synthesis in dermal fibroblasts. J Investig</br> Allergol Clin Immunol. 2008;18(4):245-52. Erratum in: J Investig Allergol Clin</br> Immunol. 2009;19(2):166. Dosage error in article text. PubMed PMID: 18714531.</br>11: Horak F, Stübner P, Zieglmayer R, Kavina A, Corrado ME, Assandri A, Mion A.</br> Clinical study of the therapeutic efficacy and safety of emedastine difumarate</br> versus cetirizine in the treatment of seasonal allergic rhinitis.</br> Arzneimittelforschung. 2004;54(10):666-72. PubMed PMID: 15553106.</br>12: Saito H, Yamamoto N, Tomita S, Taniguchi M, Hasegawa M, Akiyama K, Kawaguchi </br> H, Takahashi K. Effect of emedastine difumarate on CC chemokine-elicited</br> eosinophil migration. Int Arch Allergy Immunol. 2001;125 Suppl 1:22-8. PubMed</br> PMID: 11408768.</br>13: Secchi A, Leonardi A, Discepola M, Deschenes J, Abelson MB. An efficacy and</br> tolerance comparison of emedastine difumarate 0.05% and levocabastine</br> hydrochloride 0.05%: reducing chemosis and eyelid swelling in subjects with</br> seasonal allergic conjunctivitis. Emadine Study Group. Acta Ophthalmol Scand</br> Suppl. 2000;(230):48-51. PubMed PMID: 11057351.</br>14: el-Shazly AE, Masuyama K, Samejima Y, Eura M, Ishikawa T. Inhibition of human</br> eosinophil chemotaxis in vitro by the anti-allergic agent emedastine difumarate. </br> Immunopharmacol Immunotoxicol. 1996 Nov;18(4):587-95. PubMed PMID: 8933171.</br>15: Saito T, Hagihara A, Igarashi N, Matsuda N, Yamashita A, Ito K, Mio M, Tasaka</br> K. Inhibitory effects of emedastine difumarate on histamine release. Jpn J</br> Pharmacol. 1993 Jun;62(2):137-43. PubMed PMID: 7690432.</br>16: Sakai T, Awata N, Watanabe J. Hepatic transport of an antiallergic agent,</br> emedastine difumarate: interspecies difference in rats and guinea pigs. Chem</br> Pharm Bull (Tokyo). 1990 May;38(5):1349-52. PubMed PMID: 2393961.</br>17: Wada Y, Hamada T, Kawashima T, Awata N. [In vitro metabolism of an</br> antiallergic agent, emedastine difumarate, in rats and guinea pigs]. Yakugaku</br> Zasshi. 1990 Jan;110(1):40-8. Japanese. PubMed PMID: 1972410.</br></br>

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