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Identification
NameDipivefrin
Accession NumberDB00449  (APRD00930)
TypeSmall Molecule
GroupsApproved
DescriptionDipivefrin is a prodrug of adrenaline, which is used to treat glaucoma. It is available as ophthalmic solution (eye drops).
Structure
Thumb
Synonyms
(+-)-4-[1-Hydroxy-2-(methylamino)ethyl]-O-phenylene divavalate
1-(3',4'-Dipivaloyloxyphenyl)-2-methylamino-1-ethanol
4-[1-Hydroxy-2-(methylamino)ethyl]-O-phenylene divavalate
Dipivalyl Epinephrine
Dipivefrin
Dipivefrina
Dipivéfrine
Dipivefrinum
Pro-Epinephrine
External Identifiers
  • DPE
  • K 30081
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dipivefrin-liq Oph 0.1%Liquid.1 %OphthalmicAlcon Canada Inc1995-12-311996-08-16Canada
Dpe Ophthalmic Solution - 0.1%Solution / drops.1 %Ophthalmic; TopicalAlcon Canada Inc1995-12-311999-12-23Canada
PMS-dipivefrinSolution / drops0.1 %OphthalmicPharmascience Inc1998-08-312016-10-28Canada
Propine Liq 0.1%Liquid1 mgOphthalmicAllergan Inc1981-12-312011-08-04Canada
Ratio-dipivefrinSolution0.1 %OphthalmicRatiopharm Inc Division Of Teva Canada Limited1995-12-312006-08-04Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-dipivefrinLiquid0.1 %OphthalmicApotex Inc2000-07-17Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AKProAkorn
D EpifrinAllergan
DiopineAllergan
PivalephrineSanten Pharmaceutical
PropineAllergan
ThilodrinAlcon
Brand mixtures
NameLabellerIngredients
Probeta - Liq OphAllergan Inc
Salts
Name/CASStructureProperties
Dipivefrin Hydrochloride
64019-93-8
Thumb
  • InChI Key: VKFAUCPBMAGVRG-UHFFFAOYNA-N
  • Monoisotopic Mass: 387.181250782
  • Average Mass: 387.898
DBSALT000626
Categories
UNII8Q1PVL543G
CAS number52365-63-6
WeightAverage: 351.4373
Monoisotopic: 351.204573043
Chemical FormulaC19H29NO5
InChI KeyOCUJLLGVOUDECM-UHFFFAOYSA-N
InChI
InChI=1S/C19H29NO5/c1-18(2,3)16(22)24-14-9-8-12(13(21)11-20-7)10-15(14)25-17(23)19(4,5)6/h8-10,13,20-21H,11H2,1-7H3
IUPAC Name
2-[(2,2-dimethylpropanoyl)oxy]-5-[1-hydroxy-2-(methylamino)ethyl]phenyl 2,2-dimethylpropanoate
SMILES
CNCC(O)C1=CC(OC(=O)C(C)(C)C)=C(OC(=O)C(C)(C)C)C=C1
Pharmacology
IndicationDipivefrin is a prodrug which is used as initial therapy for the control of intraocular pressure in chronic open-angle glaucoma.
Structured Indications
PharmacodynamicsDipivefrin is a member of a class of drugs known as prodrugs. Prodrugs are usually not active in themselves and require biotransformation to the parent compound before therapeutic activity is seen. These modifications are undertaken to enhance absorption, decrease side effects and enhance stability and comfort, thus making the parent compound a more useful drug. Enhanced absorption makes the prodrug a more efficient delivery system for the parent drug because less drug will be needed to produce the desired therapeutic response. Dipivefrin is a prodrug of epinephrine formed by the diesterification of epinephrine and pivalic acid. The addition of pivaloyl groups to the epinephrine molecule enhances its lipophilic character and, as a consequence, its penetration into the anterior chamber.
Mechanism of actionDipivefrin is a prodrug with little or no pharmacologically activity until it is hydrolyzed into epinephrine inside the human eye. The liberated epinephrine, an adrenergic agonist, appears to exert its action by stimulating α -and/or β2-adrenergic receptors, leading to a decrease in aqueous production and an enhancement of outflow facility. The dipivefrin prodrug delivery system is a more efficient way of delivering the therapeutic effects of epinephrine, with fewer side effects than are associated with conventional epinephrine therapy.
TargetKindPharmacological actionActionsOrganismUniProt ID
Alpha-1A adrenergic receptorProteinyes
agonist
HumanP35348 details
Alpha-2A adrenergic receptorProteinyes
agonist
HumanP08913 details
Beta-2 adrenergic receptorProteinyes
agonist
HumanP07550 details
CholinesteraseProteinyes
potentiator
HumanP06276 details
AcetylcholinesteraseProteinunknownNot AvailableHumanP22303 details
Related Articles
AbsorptionWell absorbed following occular administration.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Dipivefrin is converted to epinephrine inside the human eye by enzyme hydrolysis.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityOral LD50 in rat is 183 mg/kg.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe risk or severity of adverse effects can be increased when 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE is combined with Dipivefrin.Experimental
AcebutololDipivefrin may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Dipivefrin.Approved, Investigational
AlprenololAlprenolol may decrease the bronchodilatory activities of Dipivefrin.Approved, Withdrawn
AmineptineAmineptine may decrease the antihypertensive activities of Dipivefrin.Illicit, Withdrawn
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Dipivefrin.Approved
Aop200704Dipivefrin may increase the atrioventricular blocking (AV block) activities of Aop200704.Investigational
ArotinololDipivefrin may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved
AtenololDipivefrin may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
AtomoxetineAtomoxetine may increase the tachycardic activities of Dipivefrin.Approved
AtosibanThe risk or severity of adverse effects can be increased when Dipivefrin is combined with Atosiban.Approved
BefunololDipivefrin may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BendroflumethiazideDipivefrin may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenmoxinThe risk or severity of adverse effects can be increased when Benmoxin is combined with Dipivefrin.Withdrawn
Benzylpenicilloyl PolylysineDipivefrin may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Betahistine.Approved
BetaxololDipivefrin may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BevantololDipivefrin may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BisoprololDipivefrin may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BopindololBopindolol may decrease the bronchodilatory activities of Dipivefrin.Approved
BromocriptineBromocriptine may increase the hypertensive activities of Dipivefrin.Approved, Investigational
BucindololDipivefrin may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolDipivefrin may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BumetanideDipivefrin may increase the hypokalemic activities of Bumetanide.Approved
BupranololBupranolol may decrease the bronchodilatory activities of Dipivefrin.Approved
CabergolineCabergoline may increase the hypertensive activities of Dipivefrin.Approved
CaroxazoneThe risk or severity of adverse effects can be increased when Caroxazone is combined with Dipivefrin.Withdrawn
CarteololCarteolol may decrease the bronchodilatory activities of Dipivefrin.Approved
CarvedilolDipivefrin may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CeliprololDipivefrin may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
ChlorothiazideDipivefrin may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorthalidoneDipivefrin may increase the hypokalemic activities of Chlorthalidone.Approved
ClomipramineClomipramine may decrease the antihypertensive activities of Dipivefrin.Approved, Vet Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Dipivefrin.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Dipivefrin.Approved
DesvenlafaxineDesvenlafaxine may increase the tachycardic activities of Dipivefrin.Approved
DihydroergotamineDihydroergotamine may increase the hypertensive activities of Dipivefrin.Approved
DosulepinDosulepin may decrease the antihypertensive activities of Dipivefrin.Approved
DoxazosinDoxazosin may decrease the vasoconstricting activities of Dipivefrin.Approved
DoxepinDoxepin may decrease the antihypertensive activities of Dipivefrin.Approved
DuloxetineDuloxetine may increase the tachycardic activities of Dipivefrin.Approved
Ergoloid mesylateErgoloid mesylate may increase the hypertensive activities of Dipivefrin.Approved
ErgonovineErgonovine may increase the hypertensive activities of Dipivefrin.Approved
ErgotamineErgotamine may increase the hypertensive activities of Dipivefrin.Approved
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Dipivefrin.Investigational
EsmololDipivefrin may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
Etacrynic acidDipivefrin may increase the hypokalemic activities of Etacrynic acid.Approved
FurazolidoneThe risk or severity of adverse effects can be increased when Furazolidone is combined with Dipivefrin.Approved, Vet Approved
FurosemideDipivefrin may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
HydracarbazineThe risk or severity of adverse effects can be increased when Hydracarbazine is combined with Dipivefrin.Approved
HydrochlorothiazideDipivefrin may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideDipivefrin may increase the hypokalemic activities of Hydroflumethiazide.Approved
ImipramineImipramine may decrease the antihypertensive activities of Dipivefrin.Approved
IndapamideDipivefrin may increase the hypokalemic activities of Indapamide.Approved
IndenololDipivefrin may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndoraminIndoramin may decrease the vasoconstricting activities of Dipivefrin.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Dipivefrin.Approved
IproclozideThe risk or severity of adverse effects can be increased when Iproclozide is combined with Dipivefrin.Withdrawn
IproniazidThe risk or severity of adverse effects can be increased when Iproniazid is combined with Dipivefrin.Withdrawn
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Dipivefrin.Approved
LabetalolDipivefrin may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LevomilnacipranLevomilnacipran may increase the tachycardic activities of Dipivefrin.Approved
MebanazineThe risk or severity of adverse effects can be increased when Mebanazine is combined with Dipivefrin.Withdrawn
MethyclothiazideDipivefrin may increase the hypokalemic activities of Methyclothiazide.Approved
Methylene blueThe risk or severity of adverse effects can be increased when Methylene blue is combined with Dipivefrin.Investigational
MetolazoneDipivefrin may increase the hypokalemic activities of Metolazone.Approved
MetoprololDipivefrin may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MianserinThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Mianserin.Approved
MilnacipranMilnacipran may increase the tachycardic activities of Dipivefrin.Approved
MinaprineThe risk or severity of adverse effects can be increased when Minaprine is combined with Dipivefrin.Approved
MirtazapineMirtazapine may decrease the antihypertensive activities of Dipivefrin.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Dipivefrin.Approved
NadololNadolol may decrease the bronchodilatory activities of Dipivefrin.Approved
NebivololNebivolol may decrease the bronchodilatory activities of Dipivefrin.Approved, Investigational
NialamideThe risk or severity of adverse effects can be increased when Nialamide is combined with Dipivefrin.Withdrawn
NortriptylineNortriptyline may decrease the antihypertensive activities of Dipivefrin.Approved
OctamoxinThe risk or severity of adverse effects can be increased when Octamoxin is combined with Dipivefrin.Withdrawn
OpipramolOpipramol may decrease the antihypertensive activities of Dipivefrin.Investigational
OxprenololOxprenolol may decrease the bronchodilatory activities of Dipivefrin.Approved
PargylineThe risk or severity of adverse effects can be increased when Pargyline is combined with Dipivefrin.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Dipivefrin.Approved, Investigational
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Dipivefrin.Approved
PheniprazineThe risk or severity of adverse effects can be increased when Pheniprazine is combined with Dipivefrin.Withdrawn
PhenoxypropazineThe risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Dipivefrin.Withdrawn
PindololPindolol may decrease the bronchodilatory activities of Dipivefrin.Approved
PiretanideDipivefrin may increase the hypokalemic activities of Piretanide.Experimental
PirlindoleThe risk or severity of adverse effects can be increased when Pirlindole is combined with Dipivefrin.Approved
PivhydrazineThe risk or severity of adverse effects can be increased when Pivhydrazine is combined with Dipivefrin.Withdrawn
PolythiazideDipivefrin may increase the hypokalemic activities of Polythiazide.Approved
PractololDipivefrin may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PrazosinPrazosin may decrease the vasoconstricting activities of Dipivefrin.Approved
PropranololPropranolol may decrease the bronchodilatory activities of Dipivefrin.Approved, Investigational
ProtriptylineProtriptyline may decrease the antihypertensive activities of Dipivefrin.Approved
QuinethazoneDipivefrin may increase the hypokalemic activities of Quinethazone.Approved
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Dipivefrin.Approved
SafrazineThe risk or severity of adverse effects can be increased when Safrazine is combined with Dipivefrin.Withdrawn
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Dipivefrin.Approved, Investigational, Vet Approved
SilodosinSilodosin may decrease the vasoconstricting activities of Dipivefrin.Approved
SotalolSotalol may decrease the bronchodilatory activities of Dipivefrin.Approved
SpironolactoneSpironolactone may decrease the vasoconstricting activities of Dipivefrin.Approved
TamsulosinTamsulosin may decrease the vasoconstricting activities of Dipivefrin.Approved, Investigational
TerazosinTerazosin may decrease the vasoconstricting activities of Dipivefrin.Approved
TianeptineTianeptine may decrease the antihypertensive activities of Dipivefrin.Approved
TimololTimolol may decrease the bronchodilatory activities of Dipivefrin.Approved
ToloxatoneThe risk or severity of adverse effects can be increased when Toloxatone is combined with Dipivefrin.Approved
TorasemideDipivefrin may increase the hypokalemic activities of Torasemide.Approved
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Dipivefrin.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Dipivefrin.Approved
TrichlormethiazideDipivefrin may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTrimazosin may decrease the vasoconstricting activities of Dipivefrin.Experimental
TrimipramineTrimipramine may decrease the antihypertensive activities of Dipivefrin.Approved
VenlafaxineVenlafaxine may increase the tachycardic activities of Dipivefrin.Approved
Food InteractionsNot Available
References
Synthesis Reference

Hussain, A. and Truelove, J.E.; U.S. Patents 3,809.714; May 7,1974; and 3,839,584; October 1, 1974; both assigned to Inter Rx Research Corp.
Henschler, D., Wagner, J. and Hampel, H.; US. Patent 4,085,270; April 18,1978; assigned to
Chemisch-Pharmazeutische Fabrik Adolf Klinge & Co. (W. Germany).

General ReferencesNot Available
External Links
ATC CodesS01EA02
AHFS Codes
  • 52:24.00
PDB EntriesNot Available
FDA labelDownload (60.3 KB)
MSDSDownload (50.2 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8575
Blood Brain Barrier-0.9747
Caco-2 permeable-0.7458
P-glycoprotein substrateSubstrate0.7499
P-glycoprotein inhibitor INon-inhibitor0.6617
P-glycoprotein inhibitor IINon-inhibitor0.7348
Renal organic cation transporterNon-inhibitor0.9396
CYP450 2C9 substrateNon-substrate0.8238
CYP450 2D6 substrateNon-substrate0.8369
CYP450 3A4 substrateNon-substrate0.5056
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9129
CYP450 3A4 inhibitorNon-inhibitor0.5546
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9757
Ames testNon AMES toxic0.9063
CarcinogenicityNon-carcinogens0.8624
BiodegradationNot ready biodegradable0.7095
Rat acute toxicity2.2818 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9635
hERG inhibition (predictor II)Non-inhibitor0.8847
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Akorn inc
  • Bausch and lomb pharmaceuticals inc
  • Falcon pharmaceuticals ltd
  • Allergan pharmaceutical
Packagers
Dosage forms
FormRouteStrength
LiquidOphthalmic0.1 %
LiquidOphthalmic.1 %
Solution / dropsOphthalmic; Topical.1 %
Solution / dropsOphthalmic0.1 %
LiquidOphthalmic
LiquidOphthalmic1 mg
SolutionOphthalmic0.1 %
Prices
Unit descriptionCostUnit
Propine 0.1% eye drops5.02USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point146-147Hussain, A. and Truelove, J.E.; U.S. Patents 3,809.714; May 7,1974; and 3,839,584; October 1, 1974; both assigned to Inter Rx Research Corp. Henschler, D., Wagner, J. and Hampel, H.; US. Patent 4,085,270; April 18,1978; assigned to Chemisch-Pharmazeutische Fabrik Adolf Klinge & Co. (W. Germany).
water solubilityFreely soluble as HCl saltNot Available
logP1.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0582 mg/mLALOGPS
logP3.17ALOGPS
logP3.71ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)14ChemAxon
pKa (Strongest Basic)9.33ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area84.86 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity94.94 m3·mol-1ChemAxon
Polarizability38.65 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenol esters. These are aromatic compounds containing a benzene ring substituted by a hydroxyl group and an ester group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol esters
Direct ParentPhenol esters
Alternative Parents
Substituents
  • Phenol ester
  • Aralkylamine
  • Dicarboxylic acid or derivatives
  • Secondary alcohol
  • Carboxylic acid ester
  • 1,2-aminoalcohol
  • Secondary amine
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot 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. Sanbe A, Tanaka Y, Fujiwara Y, Tsumura H, Yamauchi J, Cotecchia S, Koike K, Tsujimoto G, Tanoue A: Alpha1-adrenoceptors are required for normal male sexual function. Br J Pharmacol. 2007 Oct;152(3):332-40. Epub 2007 Jul 2. [PubMed:17603545 ]
  2. Tomiyama Y, Kobayashi K, Tadachi M, Kobayashi S, Inada Y, Kobayashi M, Yamazaki Y: Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter. Eur J Pharmacol. 2007 Nov 14;573(1-3):201-5. Epub 2007 Jul 6. [PubMed:17658513 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Ozakca I, Arioglu E, Guner S, Altan VM, Ozcelikay AT: Role of beta-3-adrenoceptor in catecholamine-induced relaxations in gastric fundus from control and diabetic rats. Pharmacology. 2007;80(4):227-38. Epub 2007 Jul 6. [PubMed:17622774 ]
  3. Prenner L, Sieben A, Zeller K, Weiser D, Haberlein H: Reduction of high-affinity beta2-adrenergic receptor binding by hyperforin and hyperoside on rat C6 glioblastoma cells measured by fluorescence correlation spectroscopy. Biochemistry. 2007 May 1;46(17):5106-13. Epub 2007 Apr 7. [PubMed:17417877 ]
  4. Lucin KM, Sanders VM, Jones TB, Malarkey WB, Popovich PG: Impaired antibody synthesis after spinal cord injury is level dependent and is due to sympathetic nervous system dysregulation. Exp Neurol. 2007 Sep;207(1):75-84. Epub 2007 Jun 2. [PubMed:17597612 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Nakamura M, Shirasawa E, Hikida M: Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride. Ophthalmic Res. 1993;25(1):46-51. [PubMed:8446367 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine hydrolase activity
Specific Function:
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name:
ACHE
Uniprot ID:
P22303
Molecular Weight:
67795.525 Da
References
  1. Nakamura M, Shirasawa E, Hikida M: Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride. Ophthalmic Res. 1993;25(1):46-51. [PubMed:8446367 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 08, 2016 11:11