Identification

Name
Methyldopa
Accession Number
DB00968
Description

An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. [PubChem]

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 211.2145
Monoisotopic: 211.084457909
Chemical Formula
C10H13NO4
Synonyms
  • (S)-(-)-alpha-Methyldopa
  • 3-Hydroxy-alpha-methyl-L-tyrosine
  • Alpha medopa
  • alpha-Methyl dopa
  • alpha-methyl-L-dopa
  • Alphamethyldopa
  • AMD
  • Anhydrous methyldopa
  • L-alpha-Methyldopa
  • L-Methyl Dopa
  • Methyl dopa
  • Methyldopa
  • Methyldopa anhydrous
  • metildopa
  • α-Methyl dopa
  • α-methyl-L-dopa
External IDs
  • Bayer 1440L
  • J9.247I

Pharmacology

Indication

For use in the treatment of hypertension.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. In man the antihypertensive activity appears to be due solely to the L-isomer. About twice the dose of the racemate (DL-alpha-methyldopa) is required for equal antihypertensive effect. Methyldopa has no direct effect on cardiac function and usually does not reduce glomerular filtration rate, renal blood flow, or filtration fraction. Cardiac output usually is maintained without cardiac acceleration. In some patients the heart rate is slowed. Normal or elevated plasma renin activity may decrease in the course of methyldopa therapy. Methyldopa reduces both supine and standing blood pressure. Methyldopa usually produces highly effective lowering of the supine pressure with infrequent symptomatic postural hypotension. Exercise hypotension and diurnal blood pressure variations rarely occur.

Mechanism of action

Although the mechanism of action has yet to be conclusively demonstrated, the resultant hypotensive effect is most likely due to the drug's action on the CNS. Methyldopa is converted into the metabolite, alpha-methylnorepinephrine, in the CNS, where it stimulates the central inhibitory alpha-adrenergic receptors, leading to a reduction in sympathetic tone, total peripheral resistance, and blood pressure. Reduction in plasma renin activity, as well as the inhibition of both central and peripheral norepinephrine and serotonine production may also contribute to the drug's antihypertensive effect, although this is not a major mechanism of action. This is done through the inhibition of the decarboxylation of dihydroxyphenylalanine (dopa)—the precursor of norepinephrine—and of 5-hydroxytryptophan (5-HTP)—the precursor of serotonin—in the CNS and in most peripheral tissues.

TargetActionsOrganism
AAlpha-2A adrenergic receptorNot AvailableHumans
UAromatic-L-amino-acid decarboxylase
inhibitor
Humans
Absorption

Absorption from the gastrointestinal tract is variable but averages approximately 50%.

Volume of distribution
Not Available
Protein binding

Low (less than 20%).

Metabolism

Hepatic, extensively metabolized. The known urinary metabolites are: a-methyldopa mono-0-sulfate; 3-0-methyl-a-methyldopa; 3,4-dihydroxyphenylacetone; a-methyldopamine; 3-0-methyl-a-methyldopamine and their conjugates.

Hover over products below to view reaction partners

Route of elimination

Methyldopa is extensively metabolized. The known urinary metabolites are: α-methyldopa mono-O-sulfate; 3-0-methyl-α-methyldopa; 3,4-dihydroxyphenylacetone; α-methyldopamine; 3-0-methyl-α-methyldopamine and their conjugates. Approximately 70 percent of the drug which is absorbed is excreted in the urine as methyldopa and its mono-O-sulfate conjugate. Methyldopa crosses the placental barrier, appears in cord blood, and appears in breast milk.

Half-life

The plasma half-life of methyldopa is 105 minutes.

Clearance
  • Renal cl=130 mL/min [healthy]
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

The oral LD50 of methyldopa is greater than 1.5 g/kg in both the mouse and the rat. Symptoms of overdose include bloating, constipation, diarrhea, dizziness, extreme drowsiness, gas, light-headedness, nausea, severely low blood pressure, slow heartbeat, vomiting, and weakness.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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
AbacavirMethyldopa may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarboseAcarbose may decrease the excretion rate of Methyldopa which could result in a higher serum level.
AcebutololThe therapeutic efficacy of Methyldopa can be decreased when used in combination with Acebutolol.
AceclofenacThe therapeutic efficacy of Methyldopa can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Methyldopa can be decreased when used in combination with Acemetacin.
AcetaminophenAcetaminophen may decrease the excretion rate of Methyldopa which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Methyldopa which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Methyldopa which could result in a higher serum level.
AcipimoxThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Methyldopa is combined with Acipimox.
AclidiniumMethyldopa may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Administer vitamin supplements.
  • Avoid alcohol.
  • Avoid natural licorice.
  • Take with or without food. The absorption is unaffected by food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Methyldopa hydrochloride7PX435DN5A2508-79-4QSRVZCCJDKYRRF-YDALLXLXSA-N
Methyldopa sesquihydrate56LH93261Y41372-08-1YKFCISHFRZHKHY-NGQGLHOPSA-N
Product Images
International/Other Brands
Aldomet / Aldometil / Aldomin / Dopamet / Hypolag / Medomet / Medopren / Novomedopa / Nu-Medopa
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Aldomet Ester HCl InjLiquidIntravenousMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-312002-07-29Canada flag
Aldomet Tab 125mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1971-12-311998-08-14Canada flag
Aldomet Tab 250mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-312004-11-12Canada flag
Aldomet Tab 500mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1971-12-311998-08-14Canada flag
Dopamet Tab 125mgTabletOralIcn Pharmaceuticals1976-12-312005-04-26Canada flag
Dopamet Tab 250mgTabletOralIcn Pharmaceuticals1972-12-312005-04-26Canada flag
Dopamet Tab 500mgTabletOralIcn Pharmaceuticals1976-12-312005-04-26Canada flag
Medimet 250tabTabletOralMedic Laboratory LtÉe1976-12-311996-09-09Canada flag
MethyldopaTablet125 mgOralAa Pharma Inc1980-04-02Not applicableCanada flag
MethyldopaTablet500 mgOralAa Pharma Inc1978-12-31Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MethyldopaTablet, film coated500 mg/1OralRebel Distributors1984-02-20Not applicableUS flag
MethyldopaTablet, film coated250 mg/1OralTeva Pharmaceuticals USA, Inc.2009-02-232018-02-28US flag0093 293120180814 13942 1rt80a7
MethyldopaTablet, film coated500 mg/1OralAccord Healthcare Inc.2012-07-24Not applicableUS flag16729 0031 01 nlmimage10 6440b275
MethyldopaTablet500 mg/1OralMylan Pharmaceuticals Inc.1985-04-18Not applicableUS flag
MethyldopaTablet, film coated250 mg/1OralPhysicians Total Care, Inc.1995-08-29Not applicableUS flag54868 005020180907 15195 mnoncv
MethyldopaTablet, film coated500 mg/1Oralbryant ranch prepack2012-07-242017-04-30US flag
MethyldopaTablet250 mg/1OralRemedy Repack2012-07-192013-10-22US flag00093 2931 01 nlmimage10 4a2b2559
MethyldopaTablet250 mg/1OralCardinal Health2011-08-232014-05-31US flag
MethyldopaTablet, film coated500 mg/1OralIVAX Pharmaceuticals, Inc.1986-02-201993-07-31US flag
MethyldopaTablet500 mg/1OralMylan Institutional Inc.1998-09-012020-02-29US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AldorilMethyldopa sesquihydrate (500 mg/1) + Hydrochlorothiazide (50 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31US flag
AldorilMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (15 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31US flag
AldorilMethyldopa sesquihydrate (500 mg/1) + Hydrochlorothiazide (30 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31US flag
AldorilMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (25 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31US flag
Aldoril 15 TabMethyldopa (250 mg) + Hydrochlorothiazide (15 mg)TabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1967-12-311998-08-14Canada flag
Aldoril 25 TabMethyldopa (250 mg) + Hydrochlorothiazide (25 mg)TabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-311999-03-02Canada flag
Apo Methazide 15Methyldopa (250 mg) + Hydrochlorothiazide (15 mg)TabletOralApotex Corporation1984-12-312019-05-04Canada flag
Apo Methazide 25Methyldopa (250 mg) + Hydrochlorothiazide (25 mg)TabletOralApotex Corporation1984-12-312019-05-04Canada flag
Methyldopa and HydrochlorothiazideMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (15 mg/1)TabletOralMylan Pharmaceuticals Inc.1986-01-23Not applicableUS flag
Methyldopa and HydrochlorothiazideMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralPhysicians Total Care, Inc.1986-02-152012-06-30US flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpropanoic acids. These are compounds with a structure containing a benzene ring conjugated to a propanoic acid.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Phenylpropanoic acids
Sub Class
Not Available
Direct Parent
Phenylpropanoic acids
Alternative Parents
D-alpha-amino acids / Amphetamines and derivatives / Phenylpropanes / Catechols / Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids
show 5 more
Substituents
1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / 3-phenylpropanoic-acid / Alpha-amino acid / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Amphetamine or derivatives / Aralkylamine
show 20 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
non-proteinogenic L-alpha-amino acid, L-tyrosine derivative (CHEBI:61058)

Chemical Identifiers

UNII
M4R0H12F6M
CAS number
555-30-6
InChI Key
CJCSPKMFHVPWAR-JTQLQIEISA-N
InChI
InChI=1S/C10H13NO4/c1-10(11,9(14)15)5-6-2-3-7(12)8(13)4-6/h2-4,12-13H,5,11H2,1H3,(H,14,15)/t10-/m0/s1
IUPAC Name
(2S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid
SMILES
C[[email protected]](N)(CC1=CC=C(O)C(O)=C1)C(O)=O

References

Synthesis Reference
US2868818
General References
  1. Mah GT, Tejani AM, Musini VM: Methyldopa for primary hypertension. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD003893. doi: 10.1002/14651858.CD003893.pub3. [PubMed:19821316]
  2. McCoy S, Baldwin K: Pharmacotherapeutic options for the treatment of preeclampsia. Am J Health Syst Pharm. 2009 Feb 15;66(4):337-44. doi: 10.2146/ajhp080104. [PubMed:19202042]
  3. Sica DA: Centrally acting antihypertensive agents: an update. J Clin Hypertens (Greenwich). 2007 May;9(5):399-405. [PubMed:17485976]
  4. van Zwieten PA: Development and trends in the drug treatment of essential hypertension. J Hypertens Suppl. 1992 Dec;10(7):S1-12. [PubMed:1363322]
  5. Rosenthal T, Oparil S: The effect of antihypertensive drugs on the fetus. J Hum Hypertens. 2002 May;16(5):293-8. [PubMed:12082488]
  6. van Zwieten PA, Timmermans PB: Pharmacology and characterization of central alpha-adrenoceptors involved in the effect of centrally acting antihypertensive drugs. Chest. 1983 Feb;83(2 Suppl):340-3. [PubMed:6295709]
  7. van Zwieten PA: Pharmacology of centrally acting hypotensive drugs. Br J Clin Pharmacol. 1980;10 Suppl 1:13S-20S. [PubMed:6104975]
Human Metabolome Database
HMDB0011754
KEGG Drug
D08205
KEGG Compound
C07194
PubChem Compound
38853
PubChem Substance
46508535
ChemSpider
35562
BindingDB
48449
RxNav
1545996
ChEBI
61058
ChEMBL
CHEMBL459
ZINC
ZINC000000020255
Therapeutic Targets Database
DAP000226
PharmGKB
PA450453
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Methyldopa
AHFS Codes
  • 24:08.16 — Central Alpha-agonists
FDA label
Download (155 KB)
MSDS
Download (53.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentDiabetes / Hypertensive Disease1
4CompletedTreatmentHypertension in Pregnancy / Preeclampsia1
4RecruitingPreventionHypertension, Pregnancy-Induced / Pregnancy Induced Hypertension (PIH) / Prophylaxis of preeclampsia1
4Unknown StatusDiagnosticPreeclampsia1
4Unknown StatusTreatmentPreeclampsia1
3Enrolling by InvitationTreatmentAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Orthostatic Hypotension / Orthostatic Intolerance1
2CompletedTreatmentPregnant Women With Mild Preeclampsia1
2WithdrawnPreventionType1 Diabetes Mellitus1
1Active Not RecruitingScreeningAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Orthostatic Hypotension / Orthostatic Intolerance1
1CompletedNot AvailableMyalgic Encephalomyelitis (ME) / Orthostatic Intolerance / Postural Tachycardia Syndrome1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • American Regent
  • A-S Medication Solutions LLC
  • Caremark LLC
  • Central Texas Community Health Centers
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Emcure Pharmaceuticals Ltd.
  • Endo Pharmaceuticals Inc.
  • H and H Laboratories
  • Heartland Repack Services LLC
  • Hospira Inc.
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Luitpold Pharmaceuticals Inc.
  • Major Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Watson Pharmaceuticals
Dosage Forms
FormRouteStrength
Tablet, coatedOral250 MG
Tablet, coatedOral500 MG
TabletOral283 mg
LiquidIntravenous
Tablet, film coatedOral
Tablet250 MG
TabletOral125 mg
TabletOral250 mg/1
TabletOral250 mg
TabletOral500 mg/1
TabletOral500 mg
Tablet, film coatedOral125 mg/1
Tablet, film coatedOral250 mg/1
Tablet, film coatedOral500 mg/1
TabletOral
Tablet, film coatedOral250 MG
Injection, solutionIntravenous50 mg/1mL
TabletOral
Tablet
Tablet, film coatedOral500 mg
Tablet, film coatedOral125 mg
Prices
Unit descriptionCostUnit
Aldoclor 250-250 mg tablet0.67USD tablet
Methyldopa 500 mg tablet0.67USD tablet
Methyldopa 250 mg tablet0.39USD tablet
Apo-Methyldopa 500 mg Tablet0.27USD tablet
Methyldopate 250 mg/5 ml vial0.24USD ml
Apo-Methyldopa 250 mg Tablet0.15USD tablet
Apo-Methyldopa 125 mg Tablet0.1USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)300 dec °CPhysProp
water solubility1E+004 mg/L (at 25 °C)MERCK INDEX (1996)
logP-1.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.26 mg/mLALOGPS
logP-2ALOGPS
logP-1.4ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)1.73ChemAxon
pKa (Strongest Basic)9.85ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area103.78 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity53.79 m3·mol-1ChemAxon
Polarizability20.73 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9374
Blood Brain Barrier-0.9276
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6066
P-glycoprotein inhibitor INon-inhibitor0.9852
P-glycoprotein inhibitor IINon-inhibitor0.9895
Renal organic cation transporterNon-inhibitor0.9357
CYP450 2C9 substrateNon-substrate0.7757
CYP450 2D6 substrateNon-substrate0.8
CYP450 3A4 substrateNon-substrate0.6053
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9369
CYP450 2D6 inhibitorNon-inhibitor0.9491
CYP450 2C19 inhibitorNon-inhibitor0.9233
CYP450 3A4 inhibitorNon-inhibitor0.864
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9551
Ames testNon AMES toxic0.8185
CarcinogenicityNon-carcinogens0.8997
BiodegradationNot ready biodegradable0.8077
Rat acute toxicity1.6281 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9939
hERG inhibition (predictor II)Non-inhibitor0.9629
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-MSNot Available
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-001i-0690000000-f54d986a8144f4a79b82
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0g5i-2900000000-2d1c0ec9ad93e208b620

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. 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]
  3. Sica DA: Centrally acting antihypertensive agents: an update. J Clin Hypertens (Greenwich). 2007 May;9(5):399-405. [PubMed:17485976]
  4. Kawasaki H: [Centrally acting sympathetic inhibitors for therapy of patients with hypertension]. Nihon Rinsho. 1997 Aug;55(8):2081-5. [PubMed:9284427]
  5. Head GA: Central imidazoline- and alpha 2-receptors involved in the cardiovascular actions of centrally acting antihypertensive agents. Ann N Y Acad Sci. 1999 Jun 21;881:279-86. [PubMed:10415926]
  6. van Zwieten PA: New central mediators as targets of centrally acting antihypertensive drugs. Clin Exp Hypertens. 1996 Apr-May;18(3-4):291-303. [PubMed:8743022]
  7. van Zwieten PA: Development and trends in the drug treatment of essential hypertension. J Hypertens Suppl. 1992 Dec;10(7):S1-12. [PubMed:1363322]
  8. Velliquette RA, Ernsberger P: Contrasting metabolic effects of antihypertensive agents. J Pharmacol Exp Ther. 2003 Dec;307(3):1104-11. Epub 2003 Oct 13. [PubMed:14557373]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Pyridoxal phosphate binding
Specific Function
Catalyzes the decarboxylation of L-3,4-dihydroxyphenylalanine (DOPA) to dopamine, L-5-hydroxytryptophan to serotonin and L-tryptophan to tryptamine.
Gene Name
DDC
Uniprot ID
P20711
Uniprot Name
Aromatic-L-amino-acid decarboxylase
Molecular Weight
53925.815 Da
References
  1. SOURKES TL: Inhibition of dihydroxy-phenylalanine decarboxylase by derivatives of phenylalanine. Arch Biochem Biophys. 1954 Aug;51(2):444-56. [PubMed:13189588]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 Da
References
  1. Alazizi A, Liu MY, Williams FE, Kurogi K, Sakakibara Y, Suiko M, Liu MC: Identification, characterization, and ontogenic study of a catechol O-methyltransferase from zebrafish. Aquat Toxicol. 2011 Mar;102(1-2):18-23. doi: 10.1016/j.aquatox.2010.12.016. Epub 2010 Dec 29. [PubMed:21371608]
  2. Ameyaw MM, Syvanen AC, Ulmanen I, Ofori-Adjei D, McLeod HL: Pharmacogenetics of catechol-O-methyltransferase: frequency of low activity allele in a Ghanaian population. Hum Mutat. 2000 Nov;16(5):445-6. [PubMed:11058906]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name
SLC15A1
Uniprot ID
P46059
Uniprot Name
Solute carrier family 15 member 1
Molecular Weight
78805.265 Da
References
  1. Han HK, Rhie JK, Oh DM, Saito G, Hsu CP, Stewart BH, Amidon GL: CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs. J Pharm Sci. 1999 Mar;88(3):347-50. [PubMed:10052994]

Drug created on June 13, 2005 07:24 / Updated on September 20, 2020 08:50

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