product name Loratadine
Description: Loratadine (also known as SCH29851) is a second-generation histamine H1 receptor antagonist that is used for the treatment of allergies such as allergic rhinitis and urticaria. It also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. It has been shown to inhibit the release of leukotriene C4 and histamine from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs. Loratadine is a selective inverse peripheral histamine H1-receptor agonist.
References: J Med Chem. 2014 Nov 26;57(22):9473-9; Clin Exp Allergy. 1997 May;27(5):559-67.
382.88
Formula
C22H23ClN2O2
CAS No.
79794-75-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 17 mg/mL (44.4 mM)
Water: <1 mg/mL
Ethanol: 77 mg/mL (201.1 mM)
Solubility (In vivo)
Synonyms
SCH29851
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426852
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | J Med Chem. 2014 Nov 26;57(22):9473-9; Clin Exp Allergy. 1997 May;27(5):559-67. |
