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Identification
NameNaphazoline
Accession NumberDB06711
TypeSmall Molecule
GroupsApproved
Description

Naphazoline is a rapid acting sympathomimetic vasoconstrictor of occular artierioles. It acts to decrease congestion of the conjunctiva and is found in many over-the-counter eye drops.

Structure
Thumb
Synonyms
Nafazolin
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ak-consolution/ drops1 mg/mLophthalmicPreferred Pharmaceuticals, Inc.2005-03-24Not applicableUs
Ak-consolution1 mg/mLophthalmicRebel Distributors Corp.1974-08-22Not applicableUs
Naphazolinesolution/ drops1 mg/mLophthalmicAkorn, Inc.1995-12-19Not applicableUs
Naphazolinesolution/ drops1 mg/mLophthalmicPreferred Pharmaceuticals, Inc.2013-04-22Not applicableUs
Naphazolinesolution/ drops1 mg/mLophthalmicProficient Rx LP1995-12-19Not applicableUs
Naphazolinesolution/ drops1 mg/mLophthalmicA S Medication Solutions Llc1995-12-19Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Albalondrops.1 %ophthalmicAllergan Inc1970-12-31Not applicableCanada
Clear Eyesliquid.012 %ophthalmicPrestige Brands Inc2004-03-24Not applicableCanada
Clear Eyes By Murine Eye Dpsliquid.012 %ophthalmicAbbott Laboratories, Limited1970-12-312003-10-10Canada
Diopticon Liq 0.1%liquid.1 %ophthalmicDioptic Pharmaceuticals Inc1994-12-31Not applicableCanada
Naphcon Fortesolution0.1 %ophthalmicAlcon Canada Inc1977-12-31Not applicableCanada
Nazalliquid50 mg/100mLnasalSato Pharmaceutical Co., Ltd.1990-06-11Not applicableUs
Odan-naphazolinesolution.1 %ophthalmicOdan Laboratories Ltd1986-12-31Not applicableCanada
Odan-naphazolinesolution.1 %ophthalmicOdan Laboratories Ltd1986-12-31Not applicableCanada
Opcon Oph Soln 0.1%drops.1 %ophthalmicBausch & Lomb Canada Inc.1987-12-311996-09-09Canada
Opti-tears Red Eyesolution0.1 %ophthalmicAlcon Canada IncNot applicableNot applicableCanada
Pi Yen Chinsolution/ drops1 mg/1ophthalmicInternational Nature Nutraceuticals1985-07-01Not applicableUs
Privinesuspension/ drops.125 mL/25mLnasalInsight Pharmaceuticals LLC2009-07-16Not applicableUs
Privinespray.1 mL/20mLnasalInsight Pharmaceuticals2009-07-16Not applicableUs
R.O.-naphzliquid.1 %ophthalmicRichmond Pharmaceuticals Inc.1992-12-311997-08-11Canada
Red Awayliquid.1 %ophthalmicRivex Ophthalmics Inc.1997-08-112003-07-28Canada
Redness Eye Dropsdrops0.012 %ophthalmicBausch & Lomb Inc2013-02-19Not applicableCanada
Refresh Redness Reliefsolution0.1 %ophthalmicAllergan Inc2009-02-09Not applicableCanada
Sato Clearsolution/ drops12 mg/100mLophthalmicSato Pharmaceutical Co., Ltd.1989-05-31Not applicableUs
Soothe Rednessdrops0.012 %ophthalmicBausch & Lomb Inc1988-12-31Not applicableCanada
Vasocon Eye Dropsdrops1 mgophthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1996-09-032006-08-01Canada
Vasocon Oph Soln 0.1%drops.1 %ophthalmicIolab Pharmaceuticals1988-12-311996-09-09Canada
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Advanced Eye Relief/ Redness Instant ReliefBausch & Lomb Incorporated
Advanced Eye Relief/ Redness Maximum ReliefBausch & Lomb Incorporated
Albalon AAllergan Inc
Allergy Eye DropsCVS Pharmacy
Blue CollyriumSandoz Canada Incorporated
Clear Eyes Complete 7 Symptom ReliefPrestige Brands Holdings, Inc.
Clear Eyes Complete 7 Sympton ReliefPrestige Brands Holdings, Inc.
Clear Eyes Cooling Itchy Eye ReliefPrestige Brands Holdings, Inc.
Clear Eyes Cooling Redness ReliefPrestige Brands Holdings, Inc.
Clear Eyes Maximum Itchy Eye ReliefPrestige Brands Holdings, Inc.
Clear Eyes Maximum Redness ReliefPrestige Brands Holdings, Inc.
Clear Eyes Redness ReliefPrestige Brands Holdings, Inc.
Clear Eyes Redness Relief Handy Pocket PalPrestige Brands Holdings, Inc.
Collyre BleuSabex Inc
Cooper A.R.Coopervision Inc.
Dg Health Maximum Redness ReliefDolgencorp Inc
Diopticon A LiqDioptic Pharmaceuticals Inc
Eye Allergy ReliefWalgreen Company
Eye Drops Redness and Dry Eye ReliefKc Pharmaceuticals, Inc.
Floril Redness ReliefVitaline S.A.C.
Goodsense Maximum Strength Redness Relief PlusGood Sense (Geiss, Destin & Dunn, Inc.)
Lubricant / Redness RelieverRite Aid Corporation
Lubricant and Redness RelieverTarget Corporation
Maximum Redness Relief EyeWin Co Foods, Llc
Naphazoline Hci and Pheniramine MaleateAltaire Pharmaceuticals Inc.
Naphazoline Hydrochloride and Pheniramine MaleateWalgreens
Naphcon AAlcon Laboratories, Inc.
Opcon-ABausch & Lomb Incorporated
Opti-tears AllergyAlcon Canada Inc
Optic SplashSato Pharmaceutical, Co., Ltd.
Original Redness RelieverRite Aid Corporation
Pure Eyes Sterile EyesSamson Pharmaceutical
Reactine Eye DropsMcneil Consumer Healthcare Division Of Johnson & Johnson Inc
Red Eye ReliefTarget Corporation
Refresh Eye Allergy ReliefAllergan Inc
Rhino MexLaboratoires Charton Laboratories
Rohto CoolThe Mentholatum Company
Rohto Cool MaxThe Mentholatum Company
Soothe AllergyBausch & Lomb Inc
Steritears ArLaboratoires Sterigen Inc
Vasocon A Eye DropsNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc
Vasocon A Oph SolnIolab Pharmaceuticals
Visine A Multi-action Eye Allergy ReliefJohnson & Johnson Consumer Inc.
Visine for Allergy With AntihistamineJohnson & Johnson Inc
Walgreens Maximum Redness ReliefWalgreen Company
Zincfrin AAlcon Canada Inc
Salts
Name/CASStructureProperties
Naphazoline hydrochloride
Thumb
  • InChI Key: DJDFFEBSKJCGHC-UHFFFAOYSA-N
  • Monoisotopic Mass: 246.092376197
  • Average Mass: 246.735
DBSALT000127
Categories
UNIIH231GF11BV
CAS number835-31-4
WeightAverage: 210.2744
Monoisotopic: 210.115698458
Chemical FormulaC14H14N2
InChI KeyInChIKey=CNIIGCLFLJGOGP-UHFFFAOYSA-N
InChI
InChI=1S/C14H14N2/c1-2-7-13-11(4-1)5-3-6-12(13)10-14-15-8-9-16-14/h1-7H,8-10H2,(H,15,16)
IUPAC Name
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
SMILES
C(C1=NCCN1)C1=CC=CC2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as naphthalenes. These are compounds containing a naphthalene moiety, which consists of two fused benzene rings.
KingdomOrganic compounds
Super ClassBenzenoids
ClassNaphthalenes
Sub ClassNot Available
Direct ParentNaphthalenes
Alternative Parents
Substituents
  • Naphthalene
  • Imidolactam
  • 2-imidazoline
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Carboxylic acid amidine
  • Amidine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationNaphazoline is primarily indicated in conditions like Corneal vascularity, Hyperaemia, Itching, Nasal congestion, and can also be given in adjunctive therapy as an alternative drug of choice in Sinusitis
PharmacodynamicsNaphazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion and inducing constriction around the conjunctiva. The sympathomimetic action of Naphazoline constricts the smaller arterioles of the nasal passages, producing a decongesting effect. Naphazoline ophthalmic causes constriction of blood vessels in the eyes. It also decreases itching and irritation of the eyes. aphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics.
Mechanism of actionNaphazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityExtended usage of Naphazoline can result in decreased effectiveness or a build up of tolerance against the drug. The number of receptors decreases, and when the administration of the drug is ceased, chronic congestion can occur; this is called rhinitis medicamentosa, commonly referred to as rebound congestion. Moreover long-term overdosing can cause degenerative changes in nasal mucous membranes that pose another health problem.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9936
Blood Brain Barrier+0.9693
Caco-2 permeable-0.6307
P-glycoprotein substrateSubstrate0.7448
P-glycoprotein inhibitor INon-inhibitor0.8385
P-glycoprotein inhibitor IINon-inhibitor0.6449
Renal organic cation transporterInhibitor0.8506
CYP450 2C9 substrateNon-substrate0.8202
CYP450 2D6 substrateSubstrate0.7094
CYP450 3A4 substrateNon-substrate0.7297
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.92
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9479
CYP450 3A4 inhibitorNon-inhibitor0.9206
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.889
Ames testNon AMES toxic0.8156
CarcinogenicityNon-carcinogens0.9476
BiodegradationNot ready biodegradable0.9961
Rat acute toxicity2.6904 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7043
hERG inhibition (predictor II)Non-inhibitor0.5354
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Solutionophthalmic1 mg/mL
Liquidophthalmic.012 %
Dropsophthalmic
Solution/ dropsophthalmic1 mg/mL
Solution/ dropsophthalmic
Liquidnasal50 mg/100mL
Solutionophthalmic.1 %
Dropsophthalmic.1 %
Solution/ dropsophthalmic1 mg/1
Spraynasal.1 mL/20mL
Suspension/ dropsnasal.125 mL/25mL
Liquidophthalmic.1 %
Dropsophthalmic0.012 %
Solutionophthalmic0.1 %
Liquidnasal
Liquidophthalmic
Solution/ dropsophthalmic12 mg/100mL
Dropsophthalmic1 mg
Solutionophthalmic
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0381 mg/mLALOGPS
logP3.44ALOGPS
logP2.19ChemAxon
logS-3.7ALOGPS
pKa (Strongest Basic)10.19ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area24.39 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity65.52 m3·mol-1ChemAxon
Polarizability23.77 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Roy W. Bryant, Ravi Parihar, Thomas Rowe, Susan Caballa, “Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline.” U.S. Patent US20110312998, issued December 22, 2011.

US20110312998
General ReferencesNot Available
External Links
ATC CodesR01AA08R01AB02S01GA01S01GA51
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Naphazoline.
AcetaminophenThe risk or severity of adverse effects can be increased when Naphazoline is combined with Acetaminophen.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Naphazoline is combined with Acetylsalicylic acid.
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Naphazoline.
AminophyllineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Aminophylline.
AmitriptylineAmitriptyline may increase the activities of Naphazoline.
AmphetamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Amphetamine.
ArformoterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Arformoterol.
ArmodafinilThe risk or severity of adverse effects can be increased when Naphazoline is combined with Armodafinil.
ArticaineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Articaine.
AtomoxetineAtomoxetine may increase the hypertensive activities of Naphazoline.
BenzphetamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Benzphetamine.
ButalbitalThe risk or severity of adverse effects can be increased when Naphazoline is combined with Butalbital.
CabergolineCabergoline may increase the hypertensive activities of Naphazoline.
CaffeineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Caffeine.
ChlorphentermineThe risk or severity of adverse effects can be increased when Chlorphentermine is combined with Naphazoline.
ClenbuterolThe risk or severity of adverse effects can be increased when Clenbuterol is combined with Naphazoline.
CocaineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Cocaine.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dexmethylphenidate.
DextroamphetamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dextroamphetamine.
DiethylpropionThe risk or severity of adverse effects can be increased when Naphazoline is combined with Diethylpropion.
DihydrocodeineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dihydrocodeine.
DipivefrinThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dipivefrin.
DobutamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dobutamine.
DopamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dopamine.
DoxapramThe risk or severity of adverse effects can be increased when Naphazoline is combined with Doxapram.
DoxofyllineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Doxofylline.
DronabinolDronabinol may increase the tachycardic activities of Naphazoline.
DyphyllineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Dyphylline.
EphedrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Ephedrine.
EpinephrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Epinephrine.
FenoterolThe risk or severity of adverse effects can be increased when Fenoterol is combined with Naphazoline.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Naphazoline.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Naphazoline is combined with Fluticasone Propionate.
FormoterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Formoterol.
IndacaterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Indacaterol.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Naphazoline.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Naphazoline is combined with Ipratropium bromide.
IsomethepteneThe risk or severity of adverse effects can be increased when Naphazoline is combined with Isometheptene.
IsoprenalineThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Naphazoline.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Naphazoline.
LevonordefrinThe risk or severity of adverse effects can be increased when Naphazoline is combined with Levonordefrin.
LinezolidLinezolid may increase the hypertensive activities of Naphazoline.
LisdexamfetamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Lisdexamfetamine.
MephentermineThe risk or severity of adverse effects can be increased when Mephentermine is combined with Naphazoline.
MepivacaineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Mepivacaine.
MetaraminolThe risk or severity of adverse effects can be increased when Metaraminol is combined with Naphazoline.
MethamphetamineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Methamphetamine.
MethoxamineThe risk or severity of adverse effects can be increased when Methoxamine is combined with Naphazoline.
MethylphenidateThe risk or severity of adverse effects can be increased when Naphazoline is combined with Methylphenidate.
MidodrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Midodrine.
ModafinilThe risk or severity of adverse effects can be increased when Naphazoline is combined with Modafinil.
NabiloneNabilone may increase the tachycardic activities of Naphazoline.
NorepinephrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Norepinephrine.
OlodaterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Olodaterol.
OrciprenalineThe risk or severity of adverse effects can be increased when Orciprenaline is combined with Naphazoline.
OxymetazolineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Oxymetazoline.
PhendimetrazineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Phendimetrazine.
PhenelzinePhenelzine may increase the hypertensive activities of Naphazoline.
PheniramineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Pheniramine.
PhenmetrazineThe risk or severity of adverse effects can be increased when Phenmetrazine is combined with Naphazoline.
PhentermineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Phentermine.
PhenylephrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Phenylephrine.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Naphazoline.
PirbuterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Pirbuterol.
PrazosinPrazosin may decrease the vasoconstricting activities of Naphazoline.
PropylhexedrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Propylhexedrine.
PseudoephedrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Pseudoephedrine.
RacepinephrineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Racepinephrine.
RitodrineThe risk or severity of adverse effects can be increased when Ritodrine is combined with Naphazoline.
SalbutamolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Salbutamol.
SalmeterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Salmeterol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Naphazoline.
TerbutalineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Terbutaline.
TheophyllineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Theophylline.
TranylcypromineTranylcypromine may increase the hypertensive activities of Naphazoline.
TriprolidineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Triprolidine.
VilanterolThe risk or severity of adverse effects can be increased when Naphazoline is combined with Vilanterol.
Food InteractionsNot Available

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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Bogacka E: [Decongestants in treatment of nasal obstruction]. Otolaryngol Pol. 1999;53(3):347-52. [PubMed:10481510 ]
  2. Leonardi A: Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20. [PubMed:16083326 ]
  3. Piletz JE, Zhu H, Chikkala DN: Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J Pharmacol Exp Ther. 1996 Nov;279(2):694-702. [PubMed:8930173 ]
  4. Hrometz SL, Edelmann SE, McCune DF, Olges JR, Hadley RW, Perez DM, Piascik MT: Expression of multiple alpha1-adrenoceptors on vascular smooth muscle: correlation with the regulation of contraction. J Pharmacol Exp Ther. 1999 Jul;290(1):452-63. [PubMed:10381812 ]
  5. Kai T: [Effects of topical alpha 1- and beta 2-adrenoceptor stimulants on nasal nitric oxide level]. Nihon Jibiinkoka Gakkai Kaiho. 1999 Jul;102(7):898-906. [PubMed:10459292 ]
  6. Ogidigben MJ, Chu TC, Potter DE: Naphazoline-induced suppression of aqueous humor pressure and flow: involvement of central and peripheral alpha(2)/I(1) receptors. Exp Eye Res. 2001 Mar;72(3):331-9. [PubMed:11180982 ]
Kind
Protein
Organism
Human
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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Piletz JE, Zhu H, Chikkala DN: Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J Pharmacol Exp Ther. 1996 Nov;279(2):694-702. [PubMed:8930173 ]
  2. Fukushima H, Norimoto K, Seki T, Nishiguchi T, Nakamura T, Konobu T, Nishio K, Okuchi K: Acute pulmonary edema associated with naphazoline ingestion. Clin Toxicol (Phila). 2008 Mar;46(3):254-6. [PubMed:17852165 ]
  3. Ogidigben MJ, Chu TC, Potter DE: Naphazoline-induced suppression of aqueous humor pressure and flow: involvement of central and peripheral alpha(2)/I(1) receptors. Exp Eye Res. 2001 Mar;72(3):331-9. [PubMed:11180982 ]
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Drug created on May 16, 2010 11:05 / Updated on September 16, 2013 18:04