Home Neuronal Signaling Histamine Receptor antagonist Loratadine For research use only.

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

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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
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 lnformation & 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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