Cayman Oxymetazoline (hydrochloride)

Oxymetazoline is an agonist of α₁- and α₂-adrenergic receptors (α₁- and α₂-ARs; K_ds = 6, 320, and 390 nM for α_1A-, α_1B-, and α_1D-ARs, respectively, K_i = 15 nM for α₂-AR).^, It is also an agonist of the serotonin (5-HT) receptor subtype 5-HT₁ (K_ds = 4.68, 25.7, and 5.01 nM for 5-HT_1A, 5-HT_1B, and 5-HT_1D, respectively). Oxymetazoline increases intracellular calcium levels in CHO Cells transfected with the α_1A-AR (EC₅₀ = 40.7 nM), but does not increase it measurably in cells transfected with the α_1B- or α_1D-AR (EC₅₀s = 79.4 and 240 nM, respectively). It acts as a partial agonist of the α₂-AR in isolated perfused rat heart (IC₅₀ = 63 nM and EC₅₀ = 13.5 nM for norepinephrine release).^, Oxymetazoline also acts as an agonist and antagonist of the 5-HT_1C receptor in the presence of methiothepin (K_d = 110 nM; Item No. ) and clonidine (K_d = 257 nM; Item No. ), respectively. 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-HT_1A, 5-HT_1B, 5-HT_1D receptors, respectively) and accumulation of inositol phosphates (EC₅₀ = 269 nM in pig choroid plexus preparations, which highly express 5-HT_1C receptors). Oxymetazoline (0.2 μg/kg) decreases nasal pressure in dogs by 6.9%. Formulations containing oxymetazoline have been used as nasal decongestants.

WARNING This product is not for human or veterinary use.