Home Neuronal Signaling Histamine Receptor antagonist Levocetirizine Dihydrochloride For research use only.

Levocetirizine Dihydrochloride

Synonyms: Xyzal Dihydrochloride, (-)-Cetirizine Dihydrochloride

Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.

Levocetirizine Dihydrochloride Chemical Structure

Levocetirizine Dihydrochloride Chemical Structure

CAS: 130018-87-0

Selleck's Levocetirizine Dihydrochloride has been cited by 1 publication

Purity & Quality Control

Batch: S484901 DMSO] 92 mg/mL] false] Water] 92 mg/mL] false] Ethanol] 7 mg/mL] false Purity: 99.86%
99.86

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Biological Activity

Description Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.
Targets
H1 receptor [1]
In vitro
In vitro Levocetirizine is a selective antihistaminic that acts through H1 receptor. Levocetirizine inhibits eotaxin-induced eosinophil transendothelial migration through monolayers of human dermal or lung microvascular endothelial cells in vitro. The drug also inhibits both resting and granulocyte-macrophage colony-stimulating factor (GM-CSF)-stimulated eosinophil adhesion to vascular cell adhesion molecule-1 (VCAM-1), eotaxin production by endothelial cells and ICAM-1, as well as major histocompatability complex (MHC) class I expression by interferon (IFN)-γ-stimulated keratinocytes[1].
In Vivo
In vivo In vivo, levocetirizine has rapid absorption and high bioavailability, a low potential for drug interactions, low-volume distribution and a lack of effects on cognition, psychomotor function or the cardiovascular system[1]. Levocetirizine improves renal function in diabetic rat. It attenuates the elevated renal levels of TNF-α and TGF-β1, ameliorates renal oxidative stress and restores NO bioavailability in diabetic kidney. Levocetirizine elicits vasculoprotective and renoprotective effects in experimental diabetes[2].
Animal Research Animal Models Male Sprague Dawley rats (with diabetes induced by STZ)
Dosages 0.5 mg/kg/day
Administration orally

Chemical lnformation & Solubility

Molecular Weight 461.81 Formula

C21H25ClN2O3.2HCl
CAS No. 130018-87-0 SDF --
Smiles C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 92 mg/mL

Ethanol : 7 mg/mL


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