Xylometazoline

Identification

Summary

Xylometazoline is a direct-acting alpha-adrenergic agonist used for the symptomatic treatment of nasal congestion and minor inflammation due to allergies or colds.

Generic Name
Xylometazoline
DrugBank Accession Number
DB06694
Background

Xylometazoline is an imidazoline derivative 4 with sympathomimetic and nasal decongestant activity. Xylometazoline works by binding to alpha (α)-adrenergic receptors to cause vasoconstriction of nasal blood vessels.2

Xylometazoline is available in over-the-counter (OTC) nasal sprays or drops to temporarily relieve nasal congestion due to cold, hay fever or other respiratory allergies. In some countries, it is available as combination products with ipratropium, domiphen, or dexpanthenol.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 244.3752
Monoisotopic: 244.193948778
Chemical Formula
C16H24N2
Synonyms
  • Xylometazoline
  • Xylometazolinum
  • Xylomethazoline
External IDs
  • Ba 11391
  • Ba-11391

Pharmacology

Indication

Xylometazoline is indicated for the temporary relief of nasal congestion due to cold, hay fever or other respiratory allergies.9

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination for symptomatic treatment ofAllergic rhinitis (ar)Combination Product in combination with: Ipratropium (DB00332)••••••••••••••••••••• •••••
Symptomatic treatment ofNasal congestion••• ••••••••••• • •••••• •••••
Used in combination for symptomatic treatment ofNasal congestionCombination Product in combination with: Ipratropium (DB00332)••••••••••••••••••••• •••••
Used in combination to treatNasal congestionCombination Product in combination with: Domiphen (DB11594)••• ••••••••
Used in combination for symptomatic treatment ofNasal congestionCombination Product in combination with: Dexpanthenol (DB09357)••••••••••••••••••••••• •••••• •••••••••••••••••••• ••••• •••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes.2 Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily.2,3

An early in vitro study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.8

Mechanism of action

Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow.7 As the most abundantly expressed in the human nasal mucosa, α1A- and α2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α2B-adrenoceptors,1,7 with affinity at α1A-, α2A-, α2C-, α1B-, and α1D-adrenoceptors.1 Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to oxymetazoline, another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action.7 In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.2

TargetActionsOrganism
AAlpha-2A adrenergic receptor
agonist
Humans
AAlpha-2B adrenergic receptor
agonist
Humans
AAlpha-1A adrenergic receptor
agonist
partial agonist
Humans
UAlpha-1B adrenergic receptor
agonist
Humans
UAlpha-1D adrenergic receptor
agonist
Humans
UAlpha-2C adrenergic receptor
agonist
Humans
Absorption

No information is available on xylometazoline pharmacokinetics.

Volume of distribution

No information is available on xylometazoline pharmacokinetics.

Protein binding

No information is available on xylometazoline pharmacokinetics.

Metabolism

No information is available on xylometazoline pharmacokinetics.

Route of elimination

No information is available on xylometazoline pharmacokinetics.

Half-life

No information is available on xylometazoline pharmacokinetics.

Clearance

No information is available on xylometazoline pharmacokinetics.

Adverse Effects
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Toxicity

The oral LD50 is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD50 is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD50 is 43 mg/kg in rats.11

Xylometazoline poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management.6

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Xylometazoline is combined with Acarbose.
AcebutololAcebutolol may increase the arrhythmogenic activities of Xylometazoline.
AceclofenacThe risk or severity of hypertension can be increased when Xylometazoline is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Xylometazoline is combined with Acemetacin.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Xylometazoline is combined with Acetohexamide.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Xylometazoline hydrochlorideX5S84033NZ1218-35-5YGWFCQYETHJKNX-UHFFFAOYSA-N
International/Other Brands
Balminil / Otriven / Otrivin / Otrivine / Otrix / Xylomet / Xylostar (Intas)
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
4 Way Moisturizing ReliefSpray1 mg/1mLNasalGlaxoSmithKline Consumer Healthcare Holdings (US) LLC2010-01-012017-07-27US flag
Aqua Maris Fast Acting DecongestantSpray10 mg/10mLNasalJgl North America Llc2012-12-15Not applicableUS flag
Aqua Maris Kids Fast Acting DecongestantSpray.05 mg/10mLNasalJgl North America Llc2010-09-27Not applicableUS flag
Balminil DecongestSolution0.1 %NasalTEVA Canada Limited2007-12-142021-07-30Canada flag
Balminil Nasal DecongestantSpray0.1 % w/vNasalTEVA Canada Limited1997-08-26Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
INALAR RAFFREDDOREXylometazoline hydrochloride (0.1 g/100ml) + Domiphen bromide (0.025 g/100ml)Aerosol, sprayRespiratory (inhalation)Farmakopea S.P.A.2014-07-082016-06-12Italy flag
INALAR RAFFREDDOREXylometazoline (0.1 g/100mL) + Domiphen bromide (0.025 g/100mL)SprayNasalFarmakopea S.P.A.2014-07-082022-07-02Italy flag
INALAR RAFFREDDOREXylometazoline hydrochloride (0.1 g/100ml) + Domiphen bromide (0.025 g/100ml)Aerosol, sprayRespiratory (inhalation)Farmakopea S.P.A.2014-07-082016-06-12Italy flag
nasic - Nasenspray 10 mg/500 mgXylometazoline hydrochloride (10 mg/10g) + Dexpanthenol (500 mg/10g)SprayNasalCassella Med Gmb H & Co Kg2008-10-09Not applicableAustria flag
nasic - Nasenspray für Kinder 5 mg/500 mgXylometazoline hydrochloride (5 mg/10g) + Dexpanthenol (500 mg/10g)SprayNasalCassella Med Gmb H & Co Kg2008-10-09Not applicableAustria flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Metarivin Soln. 0.1%Xylometazoline hydrochloride (1 mg/1mL)LiquidNasalLydia Co., Ltd.2022-09-30Not applicableUS flag

Categories

ATC Codes
R01AB06 — XylometazolineR01AA07 — XylometazolineS01GA53 — Xylometazoline, combinationsS01GA03 — Xylometazoline
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpropanes. These are organic compounds containing a phenylpropane moiety.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Phenylpropanes
Direct Parent
Phenylpropanes
Alternative Parents
m-Xylenes / Imidolactams / Imidazolines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Carboxamidines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
2-imidazoline / Amidine / Aromatic heteromonocyclic compound / Azacycle / Carboximidamide / Carboxylic acid amidine / Hydrocarbon derivative / Imidolactam / M-xylene / Organic 1,3-dipolar compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
alkylbenzene (CHEBI:10082)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
WPY40FTH8K
CAS number
526-36-3
InChI Key
HUCJFAOMUPXHDK-UHFFFAOYSA-N
InChI
InChI=1S/C16H24N2/c1-11-8-13(16(3,4)5)9-12(2)14(11)10-15-17-6-7-18-15/h8-9H,6-7,10H2,1-5H3,(H,17,18)
IUPAC Name
2-[(4-tert-butyl-2,6-dimethylphenyl)methyl]-4,5-dihydro-1H-imidazole
SMILES
CC1=CC(=CC(C)=C1CC1=NCCN1)C(C)(C)C

References

General 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. [Article]
  2. Eccles R, Eriksson M, Garreffa S, Chen SC: The nasal decongestant effect of xylometazoline in the common cold. Am J Rhinol. 2008 Sep-Oct;22(5):491-6. doi: 10.2500/ajr.2008.22.3202. Epub 2008 Jul 24. [Article]
  3. Graf P, Juto JE: Sustained use of xylometazoline nasal spray shortens the decongestive response and induces rebound swelling. Rhinology. 1995 Mar;33(1):14-7. [Article]
  4. Castellano F, Mautone G: Decongestant activity of a new formulation of xylometazoline nasal spray: a double-blind, randomized versus placebo and reference drugs controlled, dose-effect study. Drugs Exp Clin Res. 2002;28(1):27-35. [Article]
  5. Haldar R, Bajwa SS, Kaur J: Xylometazoline nasal drops induced anaphylaxis: An atypical perioperative complication. J Anaesthesiol Clin Pharmacol. 2017 Jul-Sep;33(3):399-401. doi: 10.4103/0970-9185.173331. [Article]
  6. Musshoff F, Madea B, Woelfle J, Vlanic D: Xylometazoline poisoning: A 40-fold nasal overdose caused by a compounding error in 3 children. Forensic Sci Int. 2014 May;238:e3-5. doi: 10.1016/j.forsciint.2014.02.011. Epub 2014 Feb 20. [Article]
  7. Eskiizmir G, Hircin Z, Ozyurt B, Unlu H: A comparative analysis of the decongestive effect of oxymetazoline and xylometazoline in healthy subjects. Eur J Clin Pharmacol. 2011 Jan;67(1):19-23. doi: 10.1007/s00228-010-0941-z. Epub 2010 Nov 11. [Article]
  8. Westerveld GJ, Scheeren RA, Dekker I, Griffioen DH, Voss HP, Bast A: Anti-oxidant actions of oxymethazoline and xylomethazoline. Eur J Pharmacol. 1995 Sep 15;291(1):27-31. doi: 10.1016/0922-4106(95)90185-x. [Article]
  9. DailyMed Label: Sinosil (xylometazoline) nasal spray [Link]
  10. Fagron: Xylometazoline Hydrochloride Safety Data Sheet [Link]
  11. Cayman Chemical: Xylometazoline Hydrochloride Safety Data Sheet [Link]
Human Metabolome Database
HMDB0015640
KEGG Drug
D08684
KEGG Compound
C07913
PubChem Compound
5709
PubChem Substance
99443248
ChemSpider
5507
BindingDB
30703
RxNav
39841
ChEBI
10082
ChEMBL
CHEMBL312448
ZINC
ZINC000000057534
PharmGKB
PA165958368
Guide to Pharmacology
GtP Drug Page
Wikipedia
Xylometazoline

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedPreventionEpistaxis1
4CompletedTreatmentCommon Cold1
4CompletedTreatmentFlexible Nasendoscopy1
4CompletedTreatmentObstructive Sleep Apnea (OSA) / Rhinitis1
4RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD) / Coronavirus Disease 2019 (COVID‑19) / Nasal Obstruction1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SprayNasal1 mg/1mL
SprayNasal1 MG/50MG/ML
SprayNasal10 mg/10mL
SprayNasal.05 mg/10mL
SprayNasal
SolutionNasal0.1 %
SprayNasal0.1 % w/v
Solution; sprayNasal0.1 %
SolutionNasal0.1 % w/v
Solution; sprayNasal.1 %
SprayNasal.1 %
Solution / dropsNasal0.1 %
Solution / dropsNasal
SprayNasal1 mg
Solution / drops; suspension / dropsNasal0.5 mg
SprayNasal0.5 mg
Solution / drops; suspension / dropsNasal1 mg
Aerosol, sprayRespiratory (inhalation)
LiquidNasal1 mg/1mL
Solution / dropsNasal0.5 MG/ML
Solution / dropsNasal1 MG/ML
GelNasal1 mg/g
SprayNasal1 MG/ML
SprayNasal0.5 MG/ML
Solution / drops; suspension / dropsNasal0.5 mg/ml
Solution / drops; suspension / dropsNasal1 mg/ml
SolutionNasal; Topical
SprayNasal10 ml
SprayNasal0.5 %
Solution / dropsOphthalmic
Solution / drops; suspension / dropsNasal0.25 mg/ml
SprayNasal0.5 mg/1ml
SprayNasal0.05 %
Solution / dropsNasal0.05 %
SprayNasal0.1 %
Liquid; sprayNasal.1 %
SolutionNasal0.5 mg/ml
SolutionNasal1 mg/ml
Solution / dropsNasal.05 %
SprayNasal.05 %
Solution / drops; suspension / dropsNasal0.1 %
SprayNasal.015 mL/15mL
SprayNasal0.1 g
SprayNasal
Spray, meteredNasal
Solution / drops; suspension / dropsNasal0.05 %
GelNasal0.1 %
Solution; sprayNasal100 mg/100mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)317-329Fagron MSDS
water solubility100 g/LFagron MSDS
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00893 mg/mLALOGPS
logP4.68ALOGPS
logP3.78Chemaxon
logS-4.4ALOGPS
pKa (Strongest Basic)10.29Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area24.39 Å2Chemaxon
Rotatable Bond Count3Chemaxon
Refractivity77.82 m3·mol-1Chemaxon
Polarizability29.87 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9866
Blood Brain Barrier+0.7293
Caco-2 permeable-0.5133
P-glycoprotein substrateSubstrate0.8254
P-glycoprotein inhibitor INon-inhibitor0.7469
P-glycoprotein inhibitor IINon-inhibitor0.8244
Renal organic cation transporterInhibitor0.6924
CYP450 2C9 substrateNon-substrate0.7815
CYP450 2D6 substrateNon-substrate0.531
CYP450 3A4 substrateNon-substrate0.5755
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9031
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9147
Ames testNon AMES toxic0.8306
CarcinogenicityNon-carcinogens0.9124
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.1884 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9218
hERG inhibition (predictor II)Non-inhibitor0.745
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-05r0-3920000000-c6f0d063c06a4d3ad4d3
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0090000000-c862fcdd09df2d7e84e1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0090000000-8a168e444e92aebe729e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0190000000-fea379e1a78158c80c57
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0490000000-f84be52191db834c336a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01s2-1950000000-6ff7d495e9ab66e5291e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01ta-1920000000-4fa30a0ba8151f6081f3
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0190000000-c880f7ffd703a6b94cc7
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0090000000-b4f6572daec9245f6002
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-00kg-9850000000-7ce3fd6c8d7e370e9863
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0940000000-e405e7f37d8f31e63733
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-054k-0920000000-78e6b3c0c95a73196f0b
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00kf-1940000000-add111b063faf4a80156
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-172.6044949
predicted
DarkChem Lite v0.1.0
[M-H]-172.0722949
predicted
DarkChem Lite v0.1.0
[M-H]-161.82759
predicted
DeepCCS 1.0 (2019)
[M+H]+173.8432949
predicted
DarkChem Lite v0.1.0
[M+H]+172.5802949
predicted
DarkChem Lite v0.1.0
[M+H]+164.1856
predicted
DeepCCS 1.0 (2019)
[M+Na]+172.8182949
predicted
DarkChem Lite v0.1.0
[M+Na]+172.3542949
predicted
DarkChem Lite v0.1.0
[M+Na]+170.27873
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
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. 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. [Article]
  2. Petrusewicz J, Kaliszan R: Effect of imidazoline drugs on human blood platelet aggregation. Thromb Haemost. 1985 Dec 17;54(4):784-7. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. 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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Partial 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. [Article]
  2. 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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]

Drug created at April 25, 2010 23:54 / Updated at February 20, 2024 23:54