Loratadine

Catalog No.S1358 Synonyms: SCH29851

Loratadine Chemical Structure

Molecular Weight(MW): 382.88

Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.

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Biological Activity

Description Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Targets
H1 receptor [1] B(0)AT2 [1]
4 μM
In vitro

Loratadine is identified as a selective inhibitor of B(0)AT2 with an IC50 of 4 μM while being less active or inactive against several other members of the SLC6 family. [1] Loratadine concentration-dependently inhibits the release of histamine and LTC4 when preincubating before Der p 1 antigen or anti-Fc epsilon RI challenge in human Fc epsilon RI+ cells. Loratadine (0.1 mM) also inhibits (10-40%) histamine, LTC4, and PGD2 release from purified HLMC (16-68%) activated by anti-Fc epsilon RI. Loratadine causes concentration-dependent inhibition (10-40%) of histamine, tryptase, LTC4, and PGD2 release from purified HSMC (24-72%) immunologically challenged with anti-Fc epsilon RI. [2] Loratadine inhibits significantly IL-6 and IL-8 secretion induced by histamine with a more powerful efficiency of the active metabolite in human umbilical vein endothelial cells (HUVEC). [3] Loratadine blocks hKv1.5 channels in a concentration-, voltage-, time- and use-dependent manner but only at concentrations much higher than therapeutic plasma levels in man in Ltk- cells transfected with the gene encoding hKv1.5 channels. [4] Loratadine inhibits rhinovirus-induced ICAM-1 upregulation in both primary bronchial or transformed (A549) respiratory epithelial cells. Loratadine also inhibits ICAM-1 mRNA induction caused by rhinovirus infection in a dose-dependent manner, and they completely inhibits rhinovirus-induced ICAM-1 promoter activation. [5]

Protocol

Solubility (25°C)

In vitro Ethanol 76 mg/mL (198.49 mM)
DMSO 17 mg/mL (44.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 382.88
Formula

C22H23ClN2O2

CAS No. 79794-75-5
Storage powder
in solvent
Synonyms SCH29851

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03196531 Completed Healthy Xian-Janssen Pharmaceutical Ltd. November 7 2017 Phase 1
NCT00751218 Completed Urticaria Merck Sharp & Dohme Corp. May 6 2004 Phase 4
NCT01673620 Completed Allergic Rhinitis Merck Sharp & Dohme Corp. July 4 2012 Phase 3
NCT03376594 Completed Allergic Rhinitis Thammasat University July 30 2017 Phase 2
NCT01916980 Completed Eczema|Dermatitis|Dermal Pruritus Merck Sharp & Dohme Corp. August 27 2013 Phase 3
NCT01916967 Completed Urticaria Merck Sharp & Dohme Corp. August 27 2013 Phase 3

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID