Alcaftadine

For research use only. Not for therapeutic Use.

  • CAT Number: A000081
  • CAS Number: 147084-10-4
  • Molecular Formula: C19H21N3O
  • Molecular Weight: 307.4
  • Purity: ≥95%
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Alcaftadine is used to prevent eye irritation brought on by allergic conjunctivitis. It is a H1 histamine receptor antagonist. It was approved by the U.S. Food and Drug Administration in 2010 under the trade name Lastacaft. Alcaftadine is an antagonist at three of the histamine receptors (1, 2 and 4). The main indication for Alcaftadine is for prevention of allergic conjunctivitis. By blocking these four receptors, Alcaftadine has been shown to significantly reduce the effects of allergens.


Catalog Number A000081
CAS Number 147084-10-4
Synonyms

Lastacaft, R89674, R 89674, R-89674

Molecular Formula C19H21N3O
Purity ≥95%
Target Neuronal Signaling
Solubility Soluble in DMSO
Storage Store at -20°C
InChI 1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
InChIKey MWTBKTRZPHJQLH-UHFFFAOYSA-N
SMILES CN1CCC(=C2C3=CC=CC=C3CCN4C2=NC=C4C=O)CC1
Reference

1: Chigbu DI, Coyne AM. Update and clinical utility of alcaftadine ophthalmic
solution 0.25% in the treatment of allergic conjunctivitis. Clin Ophthalmol. 2015
Jul 8;9:1215-25. doi: 10.2147/OPTH.S63790. eCollection 2015. Review. PubMed PMID:
26185412; PubMed Central PMCID: PMC4501164.
<br>

2: Ciolino JB, McLaurin EB, Marsico NP, Ackerman SL, Williams JM, Villanueva L,
Hollander DA. Effect of alcaftadine 0.25% on ocular itch associated with seasonal
or perennial allergic conjunctivitis: a pooled analysis of two multicenter
randomized clinical trials. Clin Ophthalmol. 2015 May 2;9:765-72. doi:
10.2147/OPTH.S80503. eCollection 2015. PubMed PMID: 25999684; PubMed Central
PMCID: PMC4427074.
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3: Pansuriya PB, Maguire GE, Friedrich HB. Synthesis and structural elucidation
of a novel polymorph of alcaftadine. Spectrochim Acta A Mol Biomol Spectrosc.
2015 May 5;142:311-9. doi: 10.1016/j.saa.2015.01.090. Epub 2015 Feb 9. PubMed
PMID: 25706601.
<br>

4: McLaurin EB, Marsico NP, Ackerman SL, Ciolino JB, Williams JM, Villanueva L,
Hollander DA. Ocular itch relief with alcaftadine 0.25% versus olopatadine 0.2%
in allergic conjunctivitis: pooled analysis of two multicenter randomized
clinical trials. Adv Ther. 2014 Oct;31(10):1059-71. doi:
10.1007/s12325-014-0155-3. Epub 2014 Sep 27. PubMed PMID: 25260889; PubMed
Central PMCID: PMC4209090.
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5: Ackerman S, D/’Ambrosio F Jr, Greiner JV, Villanueva L, Ciolino JB, Hollander
DA. A multicenter evaluation of the efficacy and duration of action of
alcaftadine 0.25% and olopatadine 0.2% in the conjunctival allergen challenge
model. J Asthma Allergy. 2013 Apr 8;6:43-52. doi: 10.2147/JAA.S38671. eCollection
2013. PubMed PMID: 24109191; PubMed Central PMCID: PMC3792834.
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6: Mahvan TD, Buckley WA, Hornecker JR. Alcaftadine for the prevention of itching
associated with allergic conjunctivitis. Ann Pharmacother. 2012
Jul-Aug;46(7-8):1025-32. doi: 10.1345/aph.1Q755. Epub 2012 Jul 17. Review. PubMed
PMID: 22811343.

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7: Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic
conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90. doi:
10.1358/dot.2011.47.12.1709243. Review. PubMed PMID: 22348913.

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8: Hussar DA, Samuel J. Vilazodone hydrochloride, linagliptin, and alcaftadine. J
Am Pharm Assoc (2003). 2011 Jul-Aug;51(4):557-9. doi: 10.1331/JAPhA.2011.11534.
PubMed PMID: 21752782.
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9: Alcaftadine (Lastacaft) for allergic conjunctivitis. Med Lett Drugs Ther. 2011
Mar 7;53(1359):19-20. PubMed PMID: 21383667.
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10: Ono SJ, Lane K. Comparison of effects of alcaftadine and olopatadine on
conjunctival epithelium and eosinophil recruitment in a murine model of allergic
conjunctivitis. Drug Des Devel Ther. 2011 Feb 8;5:77-84. doi:
10.2147/DDDT.S15788. PubMed PMID: 21340041; PubMed Central PMCID: PMC3038998.

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