Catalog No.S1358 Synonyms: SCH29851
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.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|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.|
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.  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.  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).  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.  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. 
-  Cuboni S, et al. J Med Chem, 2014, 57(22), 9473-9479.
-  Genovese A, et al. Clin Exp Allergy, 1997, 27(5), 559-567.
-  Molet S, et al. Clin Exp Allergy, 1997, 27(10), 1167-1174.
|In vitro||Ethanol||76 mg/mL (198.49 mM)|
|DMSO||17 mg/mL (44.4 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02904304||Not yet recruiting||Cold||Ache Laboratorios Farmaceuticos S.A.||August 2018||Phase 3|
|NCT03517943||Completed||Clinical Pharmacology||Bayer||April 24 2018||Phase 1|
|NCT03517930||Completed||Clinical Pharmacology||Bayer||April 17 2018||Phase 1|
|NCT03443843||Completed||Rhinitis Allergic||Bayer||February 21 2018||Phase 4|
|NCT03640273||Completed||Allergic Rhinitis|Adverse Drug Event|Quality of Life||Thammasat University||November 23 2017||Phase 2|
|NCT03196531||Completed||Healthy||Xian-Janssen Pharmaceutical Ltd.||November 7 2017||Phase 1|
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