Identification

Name
Methyldopa
Accession Number
DB00968  (APRD01106)
Type
Small Molecule
Groups
Approved
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]

Structure
Thumb
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
Product Ingredients
IngredientUNIICASInChI Key
Methyldopa hydrochloride7PX435DN5A2508-79-4QSRVZCCJDKYRRF-YDALLXLXSA-N
Methyldopa sesquihydrate56LH93261Y41372-08-1YKFCISHFRZHKHY-NGQGLHOPSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aldomet Ester HCl InjLiquid250 mgIntravenousMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-312002-07-29Canada
Aldomet Tab 125mgTablet125 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1971-12-311998-08-14Canada
Aldomet Tab 250mgTablet250 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-312004-11-12Canada
Aldomet Tab 500mgTablet500 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1971-12-311998-08-14Canada
Dopamet Tab 125mgTablet125 mgOralIcn Pharmaceuticals1976-12-312005-04-26Canada
Dopamet Tab 250mgTablet250 mgOralIcn Pharmaceuticals1972-12-312005-04-26Canada
Dopamet Tab 500mgTablet500 mgOralIcn Pharmaceuticals1976-12-312005-04-26Canada
Medimet 250tabTablet250 mgOralMedic Laboratory LtÉe1976-12-311996-09-09Canada
MethyldopaTablet125 mgOralAa Pharma Inc1980-04-02Not applicableCanada
MethyldopaTablet500 mgOralAa Pharma Inc1978-12-31Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MethyldopaTablet, film coated500 mg/1OralAccord Healthcare Limited2012-07-24Not applicableUs16729 0031 01 nlmimage10 6440b275
MethyldopaTablet, film coated250 mg/1OralPhysicians Total Care, Inc.1995-08-29Not applicableUs54868 005020180907 15195 mnoncv
MethyldopaTablet, film coated500 mg/1OralAvera McKennan Hospital2016-04-182018-06-15Us
MethyldopaTablet, film coated500 mg/1OralTeva Pharmaceuticals USA, Inc.2009-04-28Not applicableUs0093 293220180814 13942 1z117lk
MethyldopaTablet250 mg/1OralMylan Institutional1998-09-01Not applicableUs
MethyldopaTablet, film coated250 mg/1OralRebel Distributors1984-02-20Not applicableUs
MethyldopaTablet, film coated250 mg/1OralRebel Distributors2009-02-23Not applicableUs
MethyldopaTablet500 mg/1OralMylan Pharmaceuticals Inc.1985-04-18Not applicableUs
MethyldopaTablet, film coated250 mg/1OralCarilion Materials Management2012-07-24Not applicableUs
MethyldopaTablet, film coated250 mg/1OralIVAX Pharmaceuticals, Inc.1986-02-202010-09-30Us
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AldorilMethyldopa sesquihydrate (500 mg/1) + Hydrochlorothiazide (30 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31Us
AldorilMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (15 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31Us
AldorilMethyldopa sesquihydrate (500 mg/1) + Hydrochlorothiazide (50 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31Us
AldorilMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (25 mg/1)Tablet, film coatedOralMerck Sharp & Dohme Limited1962-12-202006-03-31Us
Aldoril 15 TabMethyldopa (250 mg) + Hydrochlorothiazide (15 mg)TabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1967-12-311998-08-14Canada
Aldoril 25 TabMethyldopa (250 mg) + Hydrochlorothiazide (25 mg)TabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1963-12-311999-03-02Canada
Apo Methazide 15Methyldopa (250 mg) + Hydrochlorothiazide (15 mg)TabletOralApotex Corporation1984-12-31Not applicableCanada
Apo Methazide 25Methyldopa (250 mg) + Hydrochlorothiazide (25 mg)TabletOralApotex Corporation1984-12-31Not applicableCanada
Methyldopa and HydrochlorothiazideMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralPhysicians Total Care, Inc.1986-02-152012-06-30Us
Methyldopa and HydrochlorothiazideMethyldopa sesquihydrate (250 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralMylan Pharmaceuticals Inc.1986-01-23Not applicableUs
International/Other Brands
Aldomet / Aldometil / Aldomin / Dopamet / Hypolag / Medomet / Medopren / Novomedopa / Nu-Medopa
Categories
UNII
M4R0H12F6M
CAS number
555-30-6
Weight
Average: 211.2145
Monoisotopic: 211.084457909
Chemical Formula
C10H13NO4
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[C@](N)(CC1=CC=C(O)C(O)=C1)C(O)=O

Pharmacology

Indication

For use in the treatment of hypertension.

Associated Conditions
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 AvailableHuman
UAromatic-L-amino-acid decarboxylase
inhibitor
Human
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.

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]
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
DrugInteraction
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidMethyldopa may increase the hypotensive activities of 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
3,5-DinitrocatecholThe metabolism of Methyldopa can be decreased when combined with 3,5-Dinitrocatechol.
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.
AcebutololMethyldopa may increase the hypotensive activities of 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 acidThe therapeutic efficacy of Methyldopa can be decreased when used in combination with Acetylsalicylic acid.
Food Interactions
  • Avoid alcohol.
  • Avoid natural licorice.
  • Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
  • May take Vitamin D.
  • No iron, zinc or fluoride within 2 hours of taking this medication.
  • Take without regard to meals.

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]
External Links
Human Metabolome Database
HMDB0011754
KEGG Drug
D08205
KEGG Compound
C07194
PubChem Compound
38853
PubChem Substance
46508535
ChemSpider
35562
BindingDB
48449
ChEBI
61058
ChEMBL
CHEMBL459
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
1CompletedNot AvailableMyalgic Encephalomyelitis (ME) / Orthostatic Intolerance / Postural Tachycardia Syndrome1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentAge Related Macular Degeneration (ARMD) / Neovascular Maculopathy1
1, 2WithdrawnTreatmentHigh Blood Pressure (Hypertension) / Pregnancy Toxemias / Proteinuria1
2CompletedTreatmentPregnant Women With Mild Preeclampsia1
2Not Yet RecruitingPreventionType1 Diabetes Mellitus1
3Enrolling by InvitationTreatmentAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Idiopathic orthostatic hypotension / Orthostatic Intolerance1
4CompletedTreatmentHypertension in Pregnancy / Preeclampsia1
4Not Yet RecruitingTreatmentAge Related Macular Degeneration (ARMD) / Diabetic Macular Edema (DME) / Macular Edema (ME) / Retinal Vein Occlusions(RVO)2
4RecruitingPreventionHypertension, Pregnancy-Induced / Prophylaxis of preeclampsia1
4Unknown StatusDiagnosticPreeclampsia1
4Unknown StatusTreatmentPreeclampsia1
Not AvailableActive Not RecruitingOtherPregnancy associated hypertension / Prophylaxis of preeclampsia1
Not AvailableCompletedScreeningGlaucoma1
Not AvailableCompletedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableWithdrawnTreatmentHigh Blood Pressure (Hypertension)1

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
LiquidIntravenous250 mg
Tablet, film coatedOral
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
Injection, solutionIntravenous50 mg/1mL
TabletOral
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

Taxonomy

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
3-phenylpropanoic-acid / Alpha-amino acid / D-alpha-amino acid / Alpha-amino acid or derivatives / Amphetamine or derivatives / Phenylpropane / Catechol / 1-hydroxy-2-unsubstituted benzenoid / Aralkylamine / 1-hydroxy-4-unsubstituted benzenoid
show 20 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
non-proteinogenic L-alpha-amino acid, L-tyrosine derivative (CHEBI:61058)

Targets

Kind
Protein
Organism
Human
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
Human
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
Human
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
Human
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 December 16, 2018 06:45