Uses
Adrenergic (vasoconstrictor).
Uses
Xylometazoline is used for rhinitis, laryngitis, sinusitis, inflammation of antrum of
Highmore, and allergic illnesses of the nasal cavity and throat.
Definition
ChEBI: Xylometazoline is an alkylbenzene.
brand name
Neo-Synephrine II (Sterling Winthrop); Otrivin
Hydrochloride (Ciba-Geigy).
Synthesis
Xylometazoline, 2-(4-tert-butyl-2,6-dimethylbenzyl)-2-imidazoline
(11.1.40), is also synthesized in a single reaction by cyclocondensation of 4-tert-butyl-2,6-
dimethylbenzylcyanide with ethylendiamine [43,44].
in vivo
Xylometazoline (1 mg/mL, intranasal, single dose) improves sinusitis in rats[3].
Xylometazoline and its excipients, when used for prolonged periods, may cause ophthalmic problems such as dry eyes, corneal edema, cataracts, retinal nerve fiber layer damage, and vascular damage[4].
| Animal Model: | SpragueDawley rat induced by platelet-activating factor[3] |
| Dosage: | 1 mg/mL; single dose |
| Administration: | Intranasal administration |
| Result: | Showed almost no vascular congestion, little infiltration, and the epithelium was completely intact. |
IC 50
Alpha-1A adrenergic receptor: 0.05 μM (Ki); Alpha-1B adrenergic receptor: 0.30 μM (Ki); Alpha-1D adrenergic receptor: 0.15 μM (Ki); Alpha-2A adrenergic receptor: 0.88 μM (Ki); Alpha-2B adrenergic receptor: 1.7 μM (Ki); Alpha-2C adrenergic receptor: 0.19 μM (Ki)
