Identification

Name
Oxymetazoline
Accession Number
DB00935  (APRD01158)
Type
Small Molecule
Groups
Approved, Investigational
Description

A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)

Structure
Thumb
Synonyms
  • 2-(4-Tert-butyl-2,6-dimethyl-3-hydroxybenzyl)-2-imidazoline
  • 3-[(4,5-dihydro-1H-Imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethylphenol
  • 6-t-Butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol
  • 6-Tert-butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol
  • Oximetazolinum
  • Oxymetazolina
  • Oxymetazolinum
  • Oxymethazoline
  • Oxymetozoline
Product Ingredients
IngredientUNIICASInChI Key
Oxymetazoline hydrochlorideK89MJ0S5VY2315-02-8BEEDODBODQVSIM-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clirol Nasal SpraySpray0.5 %NasalComplex Pharma Inc.Not applicableNot applicableCanada
RhofadeCream10 mg/1gTopicalAllergan, Inc.2017-01-18Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
12 Hour NasalSpray0.05 g/100mLNasalSelect Brands Distributors2000-03-01Not applicableUs
12 Hour NasalSpray0.05 g/100mLNasalAltaire Pharmaceuticals Inc.2001-06-01Not applicableUs
12 Hour NasalSpray.05 g/100mLNasalMeijer Distribution2015-05-06Not applicableUs
12 Hour NasalSpray0.05 g/100mLNasalHealthlife of Usa2018-01-02Not applicableUs
12 Hour Original Nasal DecongestantLiquid50 mg/100mLNasalPreferreed Pharmaceuticals Inc.2018-01-02Not applicableUs
12 Hour Original Nasal DecongestantLiquid50 mg/100mLNasalFaria Llc Dba Sheffield Pharmaceutcials2014-05-30Not applicableUs
7 Select NasalSpray0.05 g/100mLNasal7 Eleven2014-08-05Not applicableUs
7 Select Original NasalSpray0.05 g/1mLNasal7-ELEVEN, INC.2016-10-04Not applicableUs
AfrinSpray0.5 mg/1mLTopicalNavajo Manuracturing Company2017-12-04Not applicableUs
Afrin ColdSpray0.05 mgNasalSchering Plough2002-09-282006-08-01Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
KovanazeOxymetazoline hydrochloride (0.5 mg/1mL) + Tetracaine hydrochloride (30 mg/1mL)SprayNasalSt. Renatus2016-09-01Not applicableUs
International/Other Brands
Afrin / Dristan 12-Hour / Duramist Plus / Genasal Nasal Spray Up to 12 Hour Relief / Iliadin / Neo-Synephrine 12 Hour Spray / Nezeril / Nostrilla 12 Hour Nasal Decongestant / OcuClear / Vicks Sinex 12 Hour Nasal Spray / Vicks Sinex 12 Hour Ultra Fine Mist for Sinus Relief
Categories
UNII
8VLN5B44ZY
CAS number
1491-59-4
Weight
Average: 260.3746
Monoisotopic: 260.1888634
Chemical Formula
C16H24N2O
InChI Key
WYWIFABBXFUGLM-UHFFFAOYSA-N
InChI
InChI=1S/C16H24N2O/c1-10-8-13(16(3,4)5)15(19)11(2)12(10)9-14-17-6-7-18-14/h8,19H,6-7,9H2,1-5H3,(H,17,18)
IUPAC Name
6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol
SMILES
CC1=CC(=C(O)C(C)=C1CC1=NCCN1)C(C)(C)C

Pharmacology

Indication

For treatment of nasal congestion and redness associated with minor irritations of the eye

Associated Conditions
Pharmacodynamics

Oxymetazoline a adrenergic alpha-agonists, direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion The sympathomimetic action of oxymetazoline constricts the smaller arterioles of the nasal passages, producing a prolonged (up to 12 hours), gentle and decongesting effect. Oxymetazoline elicits relief of conjunctival hyperemia by causing vasoconstriction of superficial conjunctival blood vessels. The drug's action has been demonstrated in acute allergic conjunctivitis and in chemical (chloride) conjunctivitis.

Mechanism of action

Oxymetazoline is a direct acting sympathomimetic amine, which acts on alpha-adrenergic receptors in the arterioles of the conjunctiva and nasal mucosa. It produces vasoconstriction, resulting in decreased conjunctival congestion in ophthalmic. In nasal it produces constriction, resulting in decreased blood flow and decreased nasal congestion.

TargetActionsOrganism
AAlpha-1A adrenergic receptor
agonist
Human
AAlpha-2A adrenergic receptor
agonist
partial agonist
Human
UAlpha-2C adrenergic receptor
agonist
Human
UAlpha-2B adrenergic receptor
binder
Human
UAlpha-1B adrenergic receptor
agonist
Human
UAlpha-1D adrenergic receptor
agonist
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 4-Bromo-2,5-dimethoxyamphetamine.
6-O-benzylguanineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 6-O-benzylguanine.
7-DeazaguanineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 7-Deazaguanine.
7,9-DimethylguanineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 7,9-Dimethylguanine.
8-azaguanineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 8-azaguanine.
8-chlorotheophyllineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with 8-chlorotheophylline.
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB0015070
KEGG Compound
C07363
PubChem Compound
4636
PubChem Substance
46505622
ChemSpider
4475
BindingDB
30712
ChEBI
7862
ChEMBL
CHEMBL762
Therapeutic Targets Database
DAP000235
PharmGKB
PA164748840
IUPHAR
124
Guide to Pharmacology
GtP Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Oxymetazoline
ATC Codes
R01AA05 — OxymetazolineR01AB07 — OxymetazolineS01GA04 — Oxymetazoline
AHFS Codes
  • 52:32.00 — Vasoconstrictors
MSDS
Download (74.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAutonomic Failure / Idiopathic orthostatic hypotension1
1CompletedBasic ScienceAnaesthesia therapy1
1CompletedBasic ScienceAcute Rhinitis1
1CompletedTreatmentAllergic Rhinitis (AR)2
1CompletedTreatmentAssess Pharmacokinetics of Ketorolac Tromethamine Intranasal and Assess Effects of a Oxymetazoline Hydrochloride on the PK of Ketorolac Tromethamine / Healthy Volunteers1
1Not Yet RecruitingTreatmentIncontinence, Fecal1
1, 2CompletedTreatmentIncontinence, Fecal / Spinal Cord Injuries (SCI)1
2CompletedPreventionConjunctivitis, Seasonal Allergic1
2CompletedTreatmentAllergic Rhinitis (AR)1
2CompletedTreatmentAnaesthesia therapy3
2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
2WithdrawnTreatmentAnesthesia, Dental / Intranasal Drug Administration / Nasal Surgical Procedures1
3CompletedTreatmentAnaesthesia therapy3
3CompletedTreatmentErythemas / Rosaceas2
3CompletedTreatmentHerpes Simplex Labialis1
3RecruitingTreatmentNasal Stuffiness / Rhinitis1
3RecruitingTreatmentRosaceas1
3TerminatedTreatmentAnaesthesia therapy1
4CompletedTreatmentAdenoidal Hypertrophy1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentNasal Obstruction Present Finding1
4CompletedTreatmentRosaceas1
4Not Yet RecruitingOtherLocal Anesthetic Drug Adverse Reaction / Local Infiltration / Pulp Disease, Dental1
4RecruitingPreventionThroat Disorder1
4RecruitingTreatmentChronic Nasal Congestion / Sleep Apnea Syndrome1
4WithdrawnTreatmentAllergic Rhinitis (AR) / Rhinitis Medicamentosa / Tachyphylaxis1
Not AvailableCompletedTreatmentAdenoidectomy / Functional Endoscopic Sinus Surgery (FESS) / Turbinate Surgery1
Not AvailableCompletedTreatmentBlood Pressures / Nasal Bleeding1
Not AvailableCompletedTreatmentNasal Obstruction1
Not AvailableRecruitingBasic ScienceMiddle Ear Disease / Nasal Allergies1
Not AvailableTerminatedTreatmentChronic Rhinitis1

Pharmacoeconomics

Manufacturers
  • Schering plough healthcare products inc
  • Johnson and johnson group consumer companies
Packagers
  • Altaire Pharmaceuticals
  • Bayer Healthcare
  • Chain Drug
  • CVS Pharmacy
  • Palmetto Pharmaceuticals Inc.
  • Perrigo Co.
  • Pfizer Inc.
  • S&P Healthcare
  • Spectrum Pharmaceuticals
  • Target Corp.
  • Walgreen Co.
  • Wyeth Pharmaceuticals
Dosage forms
FormRouteStrength
LiquidNasal50 mg/100mL
SprayTopical0.5 mg/1mL
SprayNasal0.05 mg
Spray, meteredNasal0.05 g/100mL
Spray, meteredNasal0.05 mg/1mL
SprayNasal0.05 mg/100mL
SprayNasal.2 mg/.4mL
SprayNasal0.5 %
SprayNasal0.00050 g/1mL
SprayNasal
SprayNasal0.05 mg/100mg
LiquidNasal0.05 %
SprayNasal0.05 %
SolutionNasal0.05 g/100mL
SolutionNasal0.05 mg/100mL
Solution / drops; sprayNasal.025 %
SprayNasal5 g/100mL
LiquidTopical0.05 g/100mL
SprayNasal0.05 mg/1mL
Spray, meteredNasal0.0005 mL/100mL
Spray, meteredNasal0.05 mg/100mL
Solution / dropsOphthalmic.25 mg
Spray, meteredNasal0.05 %
SprayOral0.5 mg/1mL
Spray, meteredNasal0.2 mg/0.4mL
Spray, meteredNasal0.5 mg/1mL
SprayNasal50.0 mg/100.0mL
SprayNasal50 mg/100mL
CreamTopical10 mg/1g
SprayNasal7.5 mg/15mL
SprayNasal0.5 mg/1mL
SprayNasal0.05 g/100mL
SprayNasal0.512 mg/1mL
SprayNasal0.0005 g/1mL
LiquidNasal.05 %
SprayNasal0.05 g/1mL
SprayNasal0.0005055 g/1mL
SprayNasal0.0005095 g/1mL
SprayNasal0.000512 g/1mL
LiquidOphthalmic0.25 mg/1mL
LiquidOphthalmic.025 %
Solution / dropsOphthalmic0.025 %
SprayNasal.005 g/100mL
SprayNasal.05 g/100mL
SprayNasal.5 mg/1mL
SolutionNasal0.05 %
Prices
Unit descriptionCostUnit
Oxymetazoline hcl powder84.42USD g
Afrin 0.05% nose spray0.62USD ml
Drixoral cold & allergy tablet sa0.4USD tablet
Afrin no drip sinus pump mist0.38USD ml
Oxymetazoline 0.05% spray0.38USD ml
Anefrin 0.05% nasal spray0.37USD ml
Afrin sinus spray0.33USD ml
Dristan long lasting mist0.32USD ml
Neo-synephrine 12 hour spray0.28USD ml
Visine long lasting eye drops0.27USD ml
12 hour nasal relief spray0.24USD ml
Dristan cold multi-symp tablet0.23USD tablet
Ocuclear eye drops0.23USD ml
CVS Pharmacy nasal spray 0.05%0.22USD ml
No drip 0.05% nasal spray0.13USD ml
Nasal spray 0.05%0.06USD ml
Sinus nasal spray0.06USD ml
Nasal decongestant 0.05% spray0.03USD ml
Pv nasal spray 0.05%0.03USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8580282No2010-04-022030-04-02Us
US6413499No2000-03-202020-03-20Us
US9308191No2010-04-022030-04-02Us
US8883838No2011-12-012031-12-01Us
US7812049No2008-05-022028-05-02Us
US8420688No2004-08-022024-08-02Us
US9974773No2015-06-112035-06-11Us
US8815929No2004-01-222024-01-22Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)182 °CPhysProp
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0515 mg/mLALOGPS
logP3.7ALOGPS
logP3.03ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)10.91ChemAxon
pKa (Strongest Basic)10.15ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area44.62 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity79.8 m3·mol-1ChemAxon
Polarizability30.64 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9761
Blood Brain Barrier-0.5388
Caco-2 permeable-0.567
P-glycoprotein substrateSubstrate0.8858
P-glycoprotein inhibitor INon-inhibitor0.9477
P-glycoprotein inhibitor IINon-inhibitor0.6585
Renal organic cation transporterInhibitor0.6039
CYP450 2C9 substrateNon-substrate0.7585
CYP450 2D6 substrateNon-substrate0.5707
CYP450 3A4 substrateNon-substrate0.5394
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.854
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.7951
CarcinogenicityNon-carcinogens0.8923
BiodegradationNot ready biodegradable1.0
Rat acute toxicity4.4155 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8402
hERG inhibition (predictor II)Non-inhibitor0.7432
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (10.5 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as xylenols. These are aromatic compounds that contain a xylene moiety, which is a monocyclic benzene carrying exactly two methyl groups, and at least one hydroxyl group.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Xylenes
Direct Parent
Xylenols
Alternative Parents
Phenylpropanes / m-Xylenes / Para cresols / Ortho cresols / Imidolactams / Imidazolines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Carboxamidines / Azacyclic compounds
show 3 more
Substituents
Xylenol / Phenylpropane / M-xylene / O-cresol / P-cresol / Phenol / Imidolactam / 2-imidazoline / Amidine / Carboxylic acid amidine
show 12 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
phenols, carboxamidine, imidazolines (CHEBI:7862)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Yang HT, Endoh M: (+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart. Eur J Pharmacol. 1996 Oct 3;312(3):281-91. [PubMed:8894610]
  2. Deplanne V, Galzin AM: Functional characterization of alpha-1-adrenoceptor subtypes in the prostatic urethra and trigone of male rabbit. J Pharmacol Exp Ther. 1996 Aug;278(2):527-34. [PubMed:8768700]
  3. Shibata K, Taketani K: [Excitatory effect of noradrenaline on rat airway parasympathetic ganglion neurons]. Fukuoka Igaku Zasshi. 2001 Nov;92(11):377-83. [PubMed:11774707]
  4. Furukawa K, Rosario DJ, Smith DJ, Chapple CR, Uchiyama T, Chess-Williams R: Alpha 1A-adrenoceptor-mediated contractile responses of the human vas deferens. Br J Pharmacol. 1995 Sep;116(1):1605-10. [PubMed:8564226]
  5. Gonzalez-Espinosa C, Romero-Avila MT, Mora-Rodriguez DM, Gonzalez-Espinosa D, Garcia-Sainz JA: Molecular cloning and functional expression of the guinea pig alpha(1a)-adrenoceptor. Eur J Pharmacol. 2001 Aug 31;426(3):147-55. [PubMed:11527538]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
Partial agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. MacKinnon AC, Kilpatrick AT, Kenny BA, Spedding M, Brown CM: [3H]-RS-15385-197, a selective and high affinity radioligand for alpha 2-adrenoceptors: implications for receptor classification. Br J Pharmacol. 1992 Aug;106(4):1011-8. [PubMed:1327384]
  2. Mitrani P, Srinivasan M, Dodds C, Patel MS: Role of the autonomic nervous system in the development of hyperinsulinemia by high-carbohydrate formula feeding to neonatal rats. Am J Physiol Endocrinol Metab. 2007 Apr;292(4):E1069-78. Epub 2006 Dec 12. [PubMed:17164433]
  3. Lepretre N, Mironneau J: Alpha 2-adrenoceptors activate dihydropyridine-sensitive calcium channels via Gi-proteins and protein kinase C in rat portal vein myocytes. Pflugers Arch. 1994 Dec;429(2):253-61. [PubMed:7892112]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. doi: 10.1111/j.1472-8206.2009.00805.x. [PubMed:20030735]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Uhlen S, Wikberg JE: Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. [PubMed:1666366]
  2. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP: ChEMBL: a large-scale bioactivity database for drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1100-7. doi: 10.1093/nar/gkr777. Epub 2011 Sep 23. [PubMed:21948594]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. doi: 10.1111/j.1472-8206.2009.00805.x. [PubMed:20030735]
  2. Akinaga J, Lima V, Kiguti LR, Hebeler-Barbosa F, Alcantara-Hernandez R, Garcia-Sainz JA, Pupo AS: Differential phosphorylation, desensitization, and internalization of alpha1A-adrenoceptors activated by norepinephrine and oxymetazoline. Mol Pharmacol. 2013 Apr;83(4):870-81. doi: 10.1124/mol.112.082313. Epub 2013 Jan 30. [PubMed:23364786]
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP: ChEMBL: a large-scale bioactivity database for drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1100-7. doi: 10.1093/nar/gkr777. Epub 2011 Sep 23. [PubMed:21948594]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. doi: 10.1111/j.1472-8206.2009.00805.x. [PubMed:20030735]
  2. Akinaga J, Lima V, Kiguti LR, Hebeler-Barbosa F, Alcantara-Hernandez R, Garcia-Sainz JA, Pupo AS: Differential phosphorylation, desensitization, and internalization of alpha1A-adrenoceptors activated by norepinephrine and oxymetazoline. Mol Pharmacol. 2013 Apr;83(4):870-81. doi: 10.1124/mol.112.082313. Epub 2013 Jan 30. [PubMed:23364786]
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP: ChEMBL: a large-scale bioactivity database for drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1100-7. doi: 10.1093/nar/gkr777. Epub 2011 Sep 23. [PubMed:21948594]

Drug created on June 13, 2005 07:24 / Updated on October 16, 2018 08:32