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Identification
NameMethyldopa
Accession NumberDB00968  (APRD01106)
TypeSmall Molecule
GroupsApproved
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 anhydrous
α-Methyl dopa
α-methyl-L-dopa
External Identifiers
  • Bayer 1440L
Approved 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 Canada Ltd.1976-12-312005-04-26Canada
Dopamet Tab 250mgtablet250 mgoralIcn Canada Ltd.1972-12-312005-04-26Canada
Dopamet Tab 500mgtablet500 mgoralIcn Canada Ltd.1976-12-312005-04-26Canada
Medimet 250tabtablet250 mgoralMedic Laboratory LtÉe1976-12-311996-09-09Canada
Methyldopatablet125 mgoralAa Pharma Inc1980-04-02Not applicableCanada
Methyldopatablet500 mgoralAa Pharma Inc1978-12-31Not applicableCanada
Methyldopatablet250 mgoralAa Pharma Inc1976-12-31Not applicableCanada
Methyldopa 125 Tab 125mgtablet125 mgoralPro Doc Limitee1978-12-312009-07-23Canada
Methyldopa 250 Tabtablet250 mgoralPro Doc Limitee1978-12-312009-07-23Canada
Methyldopa 500 Tab 500mgtablet500 mgoralPro Doc Limitee1978-12-312009-07-23Canada
Methyldopa Tablets 125mgtablet125 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Methyldopa Tablets 250mgtablet250 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Methyldopa Tablets 500mgtablet500 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Novo-medopa Tab 125mgtablet125 mgoralNovopharm Limited1975-12-312015-10-26Canada
Novo-medopa Tab 250mgtablet250 mgoralNovopharm Limited1975-12-312015-10-26Canada
Novo-medopa Tab 500mgtablet500 mgoralNovopharm Limited1975-12-312015-10-26Canada
Nu-medopa Tab 125mgtablet125 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Nu-medopa Tab 250mgtablet250 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Nu-medopa Tab 500mgtablet500 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Methyldopatablet, film coated250 mg/1oralCarilion Materials Management2012-07-24Not applicableUs
Methyldopatablet250 mg/1oralCardinal Health2011-08-23Not applicableUs
Methyldopatablet, film coated500 mg/1oralRebel Distributors Corp1984-02-20Not applicableUs
Methyldopatablet, film coated250 mg/1oralTeva Pharmaceuticals USA Inc2009-02-23Not applicableUs
Methyldopatablet, film coated500 mg/1oralPhysicians Total Care, Inc.1996-07-26Not applicableUs
Methyldopatablet, film coated250 mg/1oralRebel Distributors Corp1984-02-20Not applicableUs
Methyldopatablet, film coated250 mg/1oralPhysicians Total Care, Inc.1995-08-29Not applicableUs
Methyldopatablet, film coated500 mg/1oralAccord Healthcare Inc.2012-06-27Not applicableUs
Methyldopatablet, film coated500 mg/1oralA S Medication Solutions Llc2009-04-28Not applicableUs
Methyldopatablet, film coated250 mg/1oralAccord Healthcare Inc.2012-06-27Not applicableUs
Methyldopatablet250 mg/1oralREMEDYREPACK INC.2012-09-25Not applicableUs
Methyldopatablet500 mg/1oralMylan Institutional Inc.1998-09-01Not applicableUs
Methyldopatablet250 mg/1oralMylan Pharmaceuticals Inc.1985-04-18Not applicableUs
Methyldopatablet250 mg/1oralMylan Institutional Inc.1998-09-01Not applicableUs
Methyldopatablet500 mg/1oralMylan Pharmaceuticals Inc.1985-04-18Not applicableUs
Methyldopatablet, film coated250 mg/1oralRebel Distributors Corp2009-02-23Not applicableUs
Methyldopatablet, film coated500 mg/1oralTeva Pharmaceuticals USA Inc2009-04-28Not applicableUs
Methyldopate Hydrochlorideinjection, solution50 mg/mLintravenousAmerican Regent, Inc.1995-09-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AldometNot Available
AldometilNot Available
AldominNot Available
DopametNot Available
HypolagNot Available
MedometNot Available
MedoprenNot Available
NovomedopaNot Available
Nu-MedopaNot Available
Brand mixtures
NameLabellerIngredients
Aldoril 15 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Aldoril 25 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Apo Methazide 15Apotex Inc
Apo Methazide 25Apotex Inc
Methyldopa and HydrochlorothiazideMylan Pharmaceuticals Inc.
Novo-doparil 15 TabNovopharm Limited
Novo-doparil 25 TabNovopharm Limited
PMS-dopazide 15 TabPharmascience Inc
PMS-dopazide-25 TabPharmascience Inc
Supres 150 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Supres 250 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Salts
Name/CASStructureProperties
Methyldopa hydrochloride
ThumbNot applicableDBSALT001139
Methyldopa sesquihydrate
41372-08-1
Thumb
  • InChI Key: YKFCISHFRZHKHY-NGQGLHOPSA-N
  • Monoisotopic Mass: 476.200609858
  • Average Mass: 476.479
DBSALT000988
Categories
UNIIM4R0H12F6M
CAS number555-30-6
WeightAverage: 211.2145
Monoisotopic: 211.084457909
Chemical FormulaC10H13NO4
InChI KeyInChIKey=CJCSPKMFHVPWAR-UEQNJFAPNA-N
InChI
InChI=1/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-/s2
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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as catecholamines and derivatives. These are compounds containing 4-(2-Aminoethyl)pyrocatechol [4-(2-aminoethyl)benzene-1,2-diol] or a derivative thereof formed by substitution.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenols and derivatives
Direct ParentCatecholamines and derivatives
Alternative Parents
Substituents
  • 3-phenylpropanoic-acid
  • Catecholamine
  • L-alpha-amino acid
  • D-alpha-amino acid
  • Amphetamine or derivatives
  • Alpha-amino acid or derivatives
  • Alpha-amino acid
  • Phenylpropane
  • Aralkylamine
  • Amino fatty acid
  • Fatty acyl
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor use in the treatment of hypertension.
PharmacodynamicsMethyldopa 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 actionAlthough 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.
Related Articles
AbsorptionAbsorption from the gastrointestinal tract is variable but averages approximately 50%.
Volume of distributionNot Available
Protein bindingLow (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.

SubstrateEnzymesProduct
Methyldopa
Not Available
3-O-methyl-a-methyldopaDetails
Methyldopa
Not Available
3-O-methyl-a-methyldopamineDetails
Methyldopa
Not Available
a-methyldopa mono-0-sulfateDetails
Methyldopa
Not Available
a-methyldopamineDetails
Route of eliminationMethyldopa 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 lifeThe plasma half-life of methyldopa is 105 minutes.
Clearance
  • Renal cl=130 mL/min [healthy]
ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Liquidintravenous250 mg
Tabletoral125 mg
Tabletoral250 mg
Tabletoral250 mg/1
Tabletoral500 mg/1
Tabletoral500 mg
Tablet, film coatedoral250 mg/1
Tablet, film coatedoral500 mg/1
Tabletoral
Injection, solutionintravenous50 mg/mL
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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point300 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 FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

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
ATC CodesNot Available
AHFS Codes
  • 24:08.16
PDB EntriesNot Available
FDA labelDownload (155 KB)
MSDSDownload (53.4 KB)
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Methyldopa.
AlfuzosinAlfuzosin may increase the hypotensive activities of Methyldopa.
AmifostineMethyldopa may increase the hypotensive activities of Amifostine.
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Methyldopa.
BretyliumBretylium may increase the bradycardic activities of Methyldopa.
BrimonidineBrimonidine may increase the antihypertensive activities of Methyldopa.
ButabarbitalButabarbital may increase the hypotensive activities of Methyldopa.
ButethalButethal may increase the hypotensive activities of Methyldopa.
CeritinibMethyldopa may increase the bradycardic activities of Ceritinib.
DiazoxideDiazoxide may increase the hypotensive activities of Methyldopa.
DuloxetineMethyldopa may increase the orthostatic hypotensive activities of Duloxetine.
EsmololEsmolol may increase the bradycardic activities of Methyldopa.
Ferric CitrateThe serum concentration of Methyldopa can be decreased when it is combined with Ferric Citrate.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Methyldopa.
HexobarbitalHexobarbital may increase the hypotensive activities of Methyldopa.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Methyldopa.
Iron DextranThe serum concentration of Methyldopa can be decreased when it is combined with Iron Dextran.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Methyldopa.
IvabradineMethyldopa may increase the bradycardic activities of Ivabradine.
LacosamideMethyldopa may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevodopaMethyldopa may increase the orthostatic hypotensive activities of Levodopa.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Methyldopa.
LithiumThe risk or severity of adverse effects can be increased when Methyldopa is combined with Lithium.
MethohexitalMethohexital may increase the hypotensive activities of Methyldopa.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Methyldopa.
MirtazapineMirtazapine may decrease the antihypertensive activities of Methyldopa.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Methyldopa.
MolsidomineMolsidomine may increase the hypotensive activities of Methyldopa.
MoxonidineMoxonidine may increase the hypotensive activities of Methyldopa.
NadololMethyldopa may increase the atrioventricular blocking (AV block) activities of Nadolol.
NicorandilNicorandil may increase the hypotensive activities of Methyldopa.
ObinutuzumabMethyldopa may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Methyldopa.
PentobarbitalPentobarbital may increase the hypotensive activities of Methyldopa.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Methyldopa.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Methyldopa.
PrimidonePrimidone may increase the hypotensive activities of Methyldopa.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Methyldopa.
QuinineQuinine may increase the hypotensive activities of Methyldopa.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Methyldopa.
RisperidoneMethyldopa may increase the hypotensive activities of Risperidone.
RituximabMethyldopa may increase the hypotensive activities of Rituximab.
RuxolitinibRuxolitinib may increase the bradycardic activities of Methyldopa.
SecobarbitalSecobarbital may increase the hypotensive activities of Methyldopa.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Methyldopa.
TadalafilTadalafil may increase the antihypertensive activities of Methyldopa.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Methyldopa.
TofacitinibTofacitinib may increase the bradycardic activities of Methyldopa.
TolcaponeThe metabolism of Methyldopa can be decreased when combined with Tolcapone.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Methyldopa.
TreprostinilTreprostinil may increase the hypotensive activities of Methyldopa.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Methyldopa.
VardenafilVardenafil may increase the antihypertensive activities of Methyldopa.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Methyldopa.
YohimbineYohimbine may decrease the antihypertensive activities of Methyldopa.
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.

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 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 ]
  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
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
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-DOPA, alpha-methyl DOPA and isoproterenol.
Gene Name:
COMT
Uniprot ID:
P21964
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
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 30, 2016 13:20