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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for symptomatic treatment of Allergic rhinitis (ar) Combination Product in combination with: Ipratropium (DB00332) •••••••••••• ••••••••• ••••• Symptomatic treatment of Nasal congestion ••• ••• •••••••• • •••••• ••••• Used in combination for symptomatic treatment of Nasal congestion Combination Product in combination with: Ipratropium (DB00332) •••••••••••• ••••••••• ••••• Used in combination to treat Nasal congestion Combination Product in combination with: Domiphen (DB11594) ••• ••• ••••• Used in combination for symptomatic treatment of Nasal congestion Combination Product in combination with: Dexpanthenol (DB09357) •••••••••••• ••••••••••• •••••• •••••••• •••••••••••• ••••• •••••••••••• ••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
Target Actions Organism AAlpha-2A adrenergic receptor agonistHumans AAlpha-2B adrenergic receptor agonistHumans AAlpha-1A adrenergic receptor agonistpartial agonistHumans UAlpha-1B adrenergic receptor agonistHumans UAlpha-1D adrenergic receptor agonistHumans UAlpha-2C adrenergic receptor agonistHumans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Xylometazoline is combined with Acarbose. Acebutolol Acebutolol may increase the arrhythmogenic activities of Xylometazoline. Aceclofenac The risk or severity of hypertension can be increased when Xylometazoline is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Xylometazoline is combined with Acemetacin. Acetohexamide The risk or severity of hypoglycemia can be increased when Xylometazoline is combined with Acetohexamide. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Xylometazoline hydrochloride X5S84033NZ 1218-35-5 YGWFCQYETHJKNX-UHFFFAOYSA-N - International/Other Brands
- Balminil / Otriven / Otrivin / Otrivine / Otrix / Xylomet / Xylostar (Intas)
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 4 Way Moisturizing Relief Spray 1 mg/1mL Nasal GlaxoSmithKline Consumer Healthcare Holdings (US) LLC 2010-01-01 2017-07-27 US Aqua Maris Fast Acting Decongestant Spray 10 mg/10mL Nasal Jgl North America Llc 2012-12-15 Not applicable US Aqua Maris Kids Fast Acting Decongestant Spray .05 mg/10mL Nasal Jgl North America Llc 2010-09-27 Not applicable US Balminil Decongest Solution 0.1 % Nasal TEVA Canada Limited 2007-12-14 2021-07-30 Canada Balminil Nasal Decongestant Spray 0.1 % w/v Nasal TEVA Canada Limited 1997-08-26 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image INALAR RAFFREDDORE Xylometazoline hydrochloride (0.1 g/100ml) + Domiphen bromide (0.025 g/100ml) Aerosol, spray Respiratory (inhalation) Farmakopea S.P.A. 2014-07-08 2016-06-12 Italy INALAR RAFFREDDORE Xylometazoline (0.1 g/100mL) + Domiphen bromide (0.025 g/100mL) Spray Nasal Farmakopea S.P.A. 2014-07-08 2022-07-02 Italy INALAR RAFFREDDORE Xylometazoline hydrochloride (0.1 g/100ml) + Domiphen bromide (0.025 g/100ml) Aerosol, spray Respiratory (inhalation) Farmakopea S.P.A. 2014-07-08 2016-06-12 Italy nasic - Nasenspray 10 mg/500 mg Xylometazoline hydrochloride (10 mg/10g) + Dexpanthenol (500 mg/10g) Spray Nasal Cassella Med Gmb H & Co Kg 2008-10-09 Not applicable Austria nasic - Nasenspray für Kinder 5 mg/500 mg Xylometazoline hydrochloride (5 mg/10g) + Dexpanthenol (500 mg/10g) Spray Nasal Cassella Med Gmb H & Co Kg 2008-10-09 Not applicable Austria - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Metarivin Soln. 0.1% Xylometazoline hydrochloride (1 mg/1mL) Liquid Nasal Lydia Co., Ltd. 2022-09-30 Not applicable US
Categories
- ATC Codes
- R01AB06 — Xylometazoline
- R01AB — Sympathomimetics, combinations excl. corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- R01AA — Sympathomimetics, plain
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- S01GA — Sympathomimetics used as decongestants
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Adrenergic Agonists
- Adrenergic alpha-1 Receptor Agonists
- Adrenergic alpha-2 Receptor Agonists
- Adrenergic alpha-Agonists
- Agents producing tachycardia
- Agents that produce hypertension
- Antiarrhythmic agents
- Antihistamine Drugs
- Calcium Channel Blockers
- Cardiovascular Agents
- Decongestants and Antiallergics
- Nasal Decongestants
- Nasal Preparations
- Ophthalmologicals
- Respiratory System Agents
- Sensory Organs
- Sympathomimetics Used as Decongestants
- Sympathomimetics, Plain
- Vasoconstrictor Agents
- Vasodilating Agents
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- DailyMed Label: Sinosil (xylometazoline) nasal spray [Link]
- Fagron: Xylometazoline Hydrochloride Safety Data Sheet [Link]
- Cayman Chemical: Xylometazoline Hydrochloride Safety Data Sheet [Link]
- External Links
- Human Metabolome Database
- HMDB0015640
- KEGG Drug
- D08684
- KEGG Compound
- C07913
- PubChem Compound
- 5709
- PubChem Substance
- 99443248
- ChemSpider
- 5507
- BindingDB
- 30703
- 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);">
Phase Status Purpose Conditions Count 4 Completed Prevention Epistaxis 1 4 Completed Treatment Common Cold 1 4 Completed Treatment Flexible Nasendoscopy 1 4 Completed Treatment Obstructive Sleep Apnea (OSA) / Rhinitis 1 4 Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) / Coronavirus Disease 2019 (COVID‑19) / Nasal Obstruction 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Spray Nasal 1 mg/1mL Spray Nasal 1 MG/50MG/ML Spray Nasal 10 mg/10mL Spray Nasal .05 mg/10mL Spray Nasal Solution Nasal 0.1 % Spray Nasal 0.1 % w/v Solution; spray Nasal 0.1 % Solution Nasal 0.1 % w/v Solution; spray Nasal .1 % Spray Nasal .1 % Solution / drops Nasal 0.1 % Solution / drops Nasal Spray Nasal 1 mg Solution / drops; suspension / drops Nasal 0.5 mg Spray Nasal 0.5 mg Solution / drops; suspension / drops Nasal 1 mg Aerosol, spray Respiratory (inhalation) Liquid Nasal 1 mg/1mL Solution / drops Nasal 0.5 MG/ML Solution / drops Nasal 1 MG/ML Gel Nasal 1 mg/g Spray Nasal 1 MG/ML Spray Nasal 0.5 MG/ML Solution / drops; suspension / drops Nasal 0.5 mg/ml Solution / drops; suspension / drops Nasal 1 mg/ml Solution Nasal; Topical Spray Nasal 10 ml Spray Nasal 0.5 % Solution / drops Ophthalmic Solution / drops; suspension / drops Nasal 0.25 mg/ml Spray Nasal 0.5 mg/1ml Spray Nasal 0.05 % Solution / drops Nasal 0.05 % Spray Nasal 0.1 % Liquid; spray Nasal .1 % Solution Nasal 0.5 mg/ml Solution Nasal 1 mg/ml Solution / drops Nasal .05 % Spray Nasal .05 % Solution / drops; suspension / drops Nasal 0.1 % Spray Nasal .015 mL/15mL Spray Nasal 0.1 g Spray Nasal Spray, metered Nasal Solution / drops; suspension / drops Nasal 0.05 % Gel Nasal 0.1 % Solution; spray Nasal 100 mg/100mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 317-329 Fagron MSDS water solubility 100 g/L Fagron MSDS logP 3.2 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00893 mg/mL ALOGPS logP 4.68 ALOGPS logP 3.78 Chemaxon logS -4.4 ALOGPS pKa (Strongest Basic) 10.29 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 24.39 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 77.82 m3·mol-1 Chemaxon Polarizability 29.87 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9866 Blood Brain Barrier + 0.7293 Caco-2 permeable - 0.5133 P-glycoprotein substrate Substrate 0.8254 P-glycoprotein inhibitor I Non-inhibitor 0.7469 P-glycoprotein inhibitor II Non-inhibitor 0.8244 Renal organic cation transporter Inhibitor 0.6924 CYP450 2C9 substrate Non-substrate 0.7815 CYP450 2D6 substrate Non-substrate 0.531 CYP450 3A4 substrate Non-substrate 0.5755 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.9031 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9147 Ames test Non AMES toxic 0.8306 Carcinogenicity Non-carcinogens 0.9124 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.1884 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9218 hERG inhibition (predictor II) Non-inhibitor 0.745
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 172.6044949 predictedDarkChem Lite v0.1.0 [M-H]- 172.0722949 predictedDarkChem Lite v0.1.0 [M-H]- 161.82759 predictedDeepCCS 1.0 (2019) [M+H]+ 173.8432949 predictedDarkChem Lite v0.1.0 [M+H]+ 172.5802949 predictedDarkChem Lite v0.1.0 [M+H]+ 164.1856 predictedDeepCCS 1.0 (2019) [M+Na]+ 172.8182949 predictedDarkChem Lite v0.1.0 [M+Na]+ 172.3542949 predictedDarkChem Lite v0.1.0 [M+Na]+ 170.27873 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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
- 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]
- 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
- 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
- AgonistPartial 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
- 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]
- 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
- 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
- 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
- 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