Loratadine

Synonyms: SCH29851

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.

Loratadine Chemical Structure

Loratadine Chemical Structure

CAS: 79794-75-5

Selleck's Loratadine has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Loratadine Related Products

Choose Selective Histamine Receptor Inhibitors

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
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05750875 Completed
Pruritus|Uremia|Chronic Kidney Diseases
King Edward Medical University
May 1 2022 Phase 4
NCT05243706 Not yet recruiting
Vinca Alkaloid Adverse Reaction
Ain Shams University
March 1 2022 Phase 3
NCT04645979 Completed
Rhinitis Allergic
Bayer
November 11 2020 --

Chemical Information & Solubility

Molecular Weight 382.88 Formula

C22H23ClN2O2

CAS No. 79794-75-5 SDF Download Loratadine SDF
Smiles CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 77 mg/mL

DMSO : 17 mg/mL ( (44.4 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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