Oxymetazoline (hydrochloride)

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Cat No: 23826

Biochemicals - Receptor Pharmacology

Oxymetazoline is an agonist of α1- and α2-adrenergic receptors (α1- and α2-ARs; Kds = 6, 320, and 390 nM for α1A-, α1B-, and α1D-ARs, respectively, Ki = 15 nM for α2-AR).{41231,41233} It is also an agonist of the serotonin (5-HT) receptor subtype 5-HT...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethyl-phenol, monohydrochloride

Correlated keywords:

1491-59-4 Afrazine Afrin Allerest Dristan Duration H 990 Iliadin Nafrine Nasivin Neo-Synephrine Nostrilla Ocuclear Oxilin Respir Sch9384

Product Overview:
Oxymetazoline is an agonist of α1- and α2-adrenergic receptors (α1- and α2-ARs; Kds = 6, 320, and 390 nM for α1A-, α1B-, and α1D-ARs, respectively, Ki = 15 nM for α2-AR).{41231,41233} 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).{41230} Oxymetazoline increases intracellular calcium levels in CHO cells transfected with the α1A-AR (EC50 = 40.7 nM), but does not increase it measurably in cells transfected with the α1B- or α1D-AR (EC50s = 79.4 and 240 nM, respectively).{41231} 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).{41228,41229} 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.{41230} 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%.{41232} Formulations containing oxymetazoline have been used as nasal decongestants.

Size	500 mg
Shipping	dry ice
CAS Number	08/02/2315 00:00
Molecular Formula	C₁₆H₂₄N₂O • HCl
SMILES	OC1=C(C)C(CC2=NCCN2)=C(C)C=C1C(C)(C)C.Cl
Molecular Weight	296,8
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2933.29
UNSPSC code	12352100

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

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