An α-AR agonist; binds to α1A-

Xylometazoline (hydrochloride) – 1 g

Brand:
Cayman
CAS:
1218-35-5
Storage:
-20
UN-No:
- /

Xylometazoline is an α-adrenergic receptor (α-AR) agonist that binds to α1A-, α1B-, α1D-, α2A-, α2B-, and α2C-ARs in a radioligand binding assay (IC50s = 0.08, 0.56, 0.45, 0.98, 1.8, and 0.22 μM, respectively).{51089} It increases intracellular calcium levels in HEK293 cells transfected with human α2B-ARs (EC50 = 99 μM) but not other α-ARs. Xylometazoline is also an agonist of the serotonin (5-HT) receptor subtype 5-HT1 (Kis = 0.7 and 14 nM for the human 5-HT1D and 5-HT1B receptors, respectively).{51090} It inhibits forskolin-induced cAMP production in CHO Pro 5 cells expressing human 5-HT1D and 5-HT1B receptors by 62 and 49%, respectively, when used at a concentration of 1 μM. Xylometazoline (0.25 μg/ml) induces contraction of isolated dog nasal mucosal blood vessels and reduces nasal patency in dogs when administered topically or intravenously.{51091}  

 

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Description

An α-AR agonist; binds to α1A-, α1B-, α1D-, α2A-, α2B-, and α2C-ARs in a radioligand binding assay (IC50s = 0.08, 0.56, 0.45, 0.98, 1.8, and 0.22 μM, respectively); increases intracellular calcium levels in HEK293 cells transfected with human α2B-ARs (EC50 = 99 μM) but not other α-ARs; a 5-HT1 receptor agonist (Kis = 0.7 and 14 nM for the human 5-HT1D and 5-HT1B receptors, respectively); inhibits forskolin-induced cAMP production in CHO Pro 5 cells expressing human 5-HT1D and 5-HT1B receptors by 62 and 49%, respectively, at 1 μM; induces contraction of isolated dog nasal mucosal blood vessels at 0.25 μg/ml; reduces nasal patency in dogs when administered topically or intravenously

Formal name: 2-[[4-(1,1-dimethylethyl)-2,6-dimethylphenyl]methyl]-4,5-dihydro-1H-imidazole, monohydrochloride

Synonyms: 

Molecular weight: 280.8

CAS: 1218-35-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation

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