Desloratadine

  • CAT Number: A000328
  • CAS Number: 100643-71-8
  • Molecular Formula: C19H19ClN2
  • Molecular Weight: 310.8
  • Purity: ≥95%
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Desloratadine (CAS 100643-71-8) is a tricyclic H1-antihistamine that is used to treat allergies. It is an active metabolite of loratadine. Desloratadine is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor; it is also an antagonist at all subtypes of the muscarinic acetylcholine receptors. It has a long-lasting effect and in moderate and low doses. It exhibits only peripheral activity since it does not readily cross the blood-brain barrier; hence, it does not cause drowsiness because it does not readily enter the central nervous system. 

Catalog Number A000328
CAS Number 100643-71-8
Molecular Formula

C19H19ClN2

Purity 95%
Target Histamine Receptor
Solubility Soluble in DMSO > 10 mM
Storage -20°C
Overview of Clinical Research

<span style="color:#000000;"><span style="font-family:arial,helvetica,sans-serif;"><span style="font-size:12px;">Desloratadine is a&nbsp;<span style="font-variant-ligatures: normal; orphans: 2; widows: 2;">Histamine H1 receptor antagonist. It has been granted for the new molecular entity.</span></span></span></span>

IUPAC Name 13-chloro-2-piperidin-4-ylidene-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
InChI InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
InChIKey JAUOIFJMECXRGI-UHFFFAOYSA-N
SMILES C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
Reference

1: Ainurofiq A, Mauludin R, Mudhakir D, Umeda D, Soewandhi SN, Putra OD, Yonemochi E. Improving mechanical properties of desloratadine via multicomponent crystal formation. Eur J Pharm Sci. 2017 Sep 27;111:65-72. doi: 10.1016/j.ejps.2017.09.035. [Epub ahead of print] PubMed PMID: 28958892.<br />
2: Zheng D, Yang X. Clinical observation on the therapeutic effect of desloratadine citrate disodium in the treatment of chronic urticaria and changes in IL4, IL18, IL23 and IL-33 levels before and after treatment. Pak J Pharm Sci. 2017 May;30(3(Special)):1139-1142. PubMed PMID: 28671097.<br />
3: Liccardi G, Calzetta L, Salzillo A, Apicella G, Cavalli F, Rogliani P. Is H1-antihistamine (desloratadine 5 mg, orodispersible tablet) premedication in NSAID-associated urticaria really safe and practicable in /real life/? J Allergy Clin Immunol Pract. 2017 Mar – Apr;5(2):535. doi: 10.1016/j.jaip.2016.12.019. PubMed PMID: 28283171.<br />
4: Staevska MT. Comparative efficacy of bilastine, levocetirizine and desloratadine updosing in chronic urticaria. Ther Clin Risk Manag. 2016 Nov 25;12:1793-1796. eCollection 2016. PubMed PMID: 27932886; PubMed Central PMCID: PMC5135004.<br />
5: Li J, Guo A, Chen W, Bin L, He Y, Zhu W, Peng C, Yan S, Chen M, Zhang J, Su J, Yi M, Liu Z, Zhang W, Zeng W, Leung DY, Chen X. Association of ORAI1 gene polymorphisms with chronic spontaneous urticaria and the efficacy of the nonsedating H1 antihistamine desloratadine. J Allergy Clin Immunol. 2017 Apr;139(4):1386-1388.e9. doi: 10.1016/j.jaci.2016.10.017. Epub 2016 Nov 15. PubMed PMID: 27864023.<br />
6: Antonijoan R, Coimbra J, Garc&iacute;a-Gea C, Puntes M, Gich I, Campo C, Valiente R, Labeaga L. Comparative efficacy of bilastine, desloratadine and rupatadine in the suppression of wheal and flare response induced by intradermal histamine in healthy volunteers. Curr Med Res Opin. 2017 Jan;33(1):129-136. Epub 2016 Oct 21. PubMed PMID: 27659218.<br />
7: Munoz-Cano R, Ainsua-Enrich E, Torres-Atencio I, Martin M, S&aacute;nchez-Lopez J, Bartra J, Picado C, Mullol J, Valero A. Effects of Rupatadine on Platelet- Activating Factor-Induced Human Mast Cell Degranulation Compared With Desloratadine and Levocetirizine (The MASPAF Study). J Investig Allergol Clin Immunol. 2017;27(3):161-168. doi: 10.18176/jiaci.0117. Epub 2016 Oct 19. PubMed PMID: 27758758.<br />
8: Wandalsen GF, Miranda C, Ensina LF, Sano F, Amazonas RB, Silva JMD, Sol&eacute; D. Association between desloratadine and prednisolone in the treatment of children with acute symptoms of allergic rhinitis: a double-blind, randomized and controlled clinical trial. Braz J Otorhinolaryngol. 2016 Sep 13. pii: S1808-8694(16)30173-2. doi: 10.1016/j.bjorl.2016.08.009. [Epub ahead of print] PubMed PMID: 27670203.<br />
9: Wang R, Zhang C. [Clinical evaluation of Montelukast plus Budesonide nasal spray and Desloratadine citrate disodium in treating moderate and severe persistent allergic rhinitis]. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2015 Dec;29(23):2041-3. Chinese. PubMed PMID: 27101674.<br />
10: Szakonyi G, Zelk&oacute; R. Carbopol&reg;-crospovidone interpolymer complex for pH-dependent desloratadine release. J Pharm Biomed Anal. 2016 May 10;123:141-6. doi: 10.1016/j.jpba.2016.02.012. Epub 2016 Feb 12. PubMed PMID: 26897295.

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