| Vasoconstrictor, used as a nasal decongestant. An ingredient of Drixin. Oxymetazoline is an agonist of alpha1- and alpha2-adrenergic receptors (alpha1- and alpha2-ARs, Kds = 6, 320, and 390 nM for alpha1A-, alpha1B-, and alpha1D-ARs, respectively, Ki = 15 nM for alpha2-AR).1,2 It is also an agonist of the serotonin (5-HT) receptor subtype 5-HT1 (Kds = 4.68, 25.7, and 5.01 nM for 5-HT1A, 5-HT1B, and 5-HT1D, respectively).3 Oxymetazoline increases intracellular calcium levels in CHO cells transfected with the alpha1A-AR (EC50 = 40.7 nM), but does not increase it measurably in cells transfected with the alpha1B- or alpha1D-AR (EC50s = 79.4 and 240 nM, respectively).1 It acts as a partial agonist of the alpha2-AR in isolated perfused rat heart (IC50 = 63 nM and EC50 = 13.5 nM for norepinephrine release).4,5 Oxymetazoline also acts as an agonist and antagonist of the 5-HT1C receptor in the presence of methiothepin (Kd = 110 nM, Item No. 23138) and clonidine (Kd = 257 nM, Item No. 15949), respectively.3 In functional second messenger assays, oxymetazoline inhibits forskolin-stimulated adenylate cyclase activity (EC50s = 18.6, 24.0, and 44.7 nM in tissues expressing high levels of 5-HT1A, 5-HT1B, 5-HT1D receptors, respectively) and accumulation of inositol phosphates (EC50 = 269 nM in pig choroid plexus preparations, which highly express 5-HT1C receptors). Oxymetazoline (0.2 µg/kg) decreases nasal pressure in dogs by 6.9%.6 Formulations containing oxymetazoline have been used as nasal decongestants. Synonyms: 3-[(4,5-Dihydro-1H-imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethylphenol Hydrochloride, 2-(4-tert-Butyl-2,6-dimethyl-3-hydroxybenzyl)-2-imidazoline Hydrochloride, 6-tert-Butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol Hydrochloride, Hazol, Navasin, Navisin, Nezeril, Oxylazine, Rhinofrenol, Rhinolitan, Sinerol CAS No: 2315-02-8 1491-59-4-free base Molecular Formula: C16H25ClN2O Molecular Weight: 296.84 Appearance: White to off-white, pale yellow solid Purity: 99% (HPLC) Melting Point: >270C (dec.) Solubility: DMSO, Methanol, Water Storage: 4C |
