Identification

Summary

Ritodrine is an adrenergic beta agonist used to treat premature labor.

Generic Name
Ritodrine
DrugBank Accession Number
DB00867
Background

Adrenergic beta-agonist used to control premature labor.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 287.359
Monoisotopic: 287.15214354
Chemical Formula
C17H21NO3
Synonyms
  • p-Hydroxy-alpha-(1-((p-hydroxyphenethyl)amino)ethyl)benzyl alcohol
  • Ritodrina
  • Ritodrine
  • Ritodrinium
External IDs
  • DU-21220

Pharmacology

Indication

For the treatment and prophylaxis of premature labour

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Beta-2 adrenergic receptors are located at sympathetic neuroeffector junctions of many organs, including uterus. Ritodrine is beta-2 adrenergic agonist. It stimulates beta-2 adrenergic receptor, increases cAMP level and decreases intracellular calcium concentration. The decrease of calcium concentration leads to a relaxation of uterine smooth muscle and, therefore, a decrease in premature uterine contractions.

Mechanism of action

Ritodrine is beta-2 adrenergic agonist. It binds to beta-2 adrenergic receptors on outer membrane of myometrial cell, activates adenyl cyclase to increase the level of cAMP which decreases intracellular calcium and leads to a decrease of uterine contractions.

TargetActionsOrganism
ABeta-2 adrenergic receptor
agonist
Humans
ABeta adrenergic receptor
agonist
downregulator
Humans
AATP-sensitive potassium channel
activator
Humans
UCalcium transporting ATPases
inhibitor
Humans
ACalcium-activated potassium channel
activator
Humans
UMyosin light chain kinase, smooth muscle
inhibitor
Humans
USulfotransferase 1C4
substrate
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

~56%

Metabolism

Hepatic, by both the mother and fetus

Route of elimination

Not Available

Half-life

1.7-2.6 hours

Clearance

Not Available

Adverse Effects
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Toxicity

LD50=64mg/kg (mice, IV); LD50=540 mg/kg (mice, oral); LD50=85 mg/kg (rat, IV)

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
AbaloparatideThe risk or severity of adverse effects can be increased when Ritodrine is combined with Abaloparatide.
AcebutololThe therapeutic efficacy of Ritodrine can be decreased when used in combination with Acebutolol.
AceclofenacThe risk or severity of hypertension can be increased when Ritodrine is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Ritodrine is combined with Acemetacin.
Acetylsalicylic acidThe risk or severity of hypertension can be increased when Ritodrine is combined with Acetylsalicylic acid.
AclidiniumThe risk or severity of Tachycardia can be increased when Ritodrine is combined with Aclidinium.
AdenosineThe risk or severity of Tachycardia can be increased when Adenosine is combined with Ritodrine.
AlclofenacThe risk or severity of hypertension can be increased when Ritodrine is combined with Alclofenac.
AlfentanilThe risk or severity of hypertension can be increased when Alfentanil is combined with Ritodrine.
AlfuzosinThe therapeutic efficacy of Ritodrine can be decreased when used in combination with Alfuzosin.
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Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Ritodrine hydrochlorideESJ56Q60GC23239-51-2IDLSITKDRVDKRV-JSUROZADSA-N
International/Other Brands
Yutopar
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Yutopar Inj 50mg/5mlLiquid10 mg / mLIntravenousBristol Labs Division Of Bristol Myers Squibb1984-12-312001-07-30Canada flag
Yutopar Tab 10mgTablet10 mg / tabOralBristol Labs Division Of Bristol Myers Squibb1984-12-312001-07-30Canada flag

Categories

ATC Codes
G02CA01 — Ritodrine
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
I0Q6O6740J
CAS number
26652-09-5
InChI Key
IOVGROKTTNBUGK-SJKOYZFVSA-N
InChI
InChI=1S/C17H21NO3/c1-12(17(21)14-4-8-16(20)9-5-14)18-11-10-13-2-6-15(19)7-3-13/h2-9,12,17-21H,10-11H2,1H3/t12-,17-/m1/s1
IUPAC Name
4-[(1S,2R)-1-hydroxy-2-{[2-(4-hydroxyphenyl)ethyl]amino}propyl]phenol
SMILES
C[C@@H](NCCC1=CC=C(O)C=C1)[C@@H](O)C1=CC=C(O)C=C1

References

Synthesis Reference

Naoki Yamazaki, Yoshimasa Fukuda, Yoshiaki Shibazaki, Tetsutarou Niizato, Isao Kosugi, Shin Yoshioka, "(-)-ritodrine, therapeutic compositions and use, and method of preparation." U.S. Patent US5449694, issued July, 1992.

US5449694
General References
Not Available
Human Metabolome Database
HMDB0015005
KEGG Drug
D02359
KEGG Compound
C07239
PubChem Compound
33572
PubChem Substance
46505273
ChemSpider
599993
BindingDB
50493311
RxNav
9392
ChEBI
156577
ChEMBL
CHEMBL489553
ZINC
ZINC000000057483
Therapeutic Targets Database
DAP000937
PharmGKB
PA451258
Drugs.com
Drugs.com Drug Page
Wikipedia
Ritodrine
MSDS
Download (48 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionPremature Births1
4Unknown StatusPreventionPreterm Labor Without Delivery1
1CompletedTreatmentHealthy Subjects (HS)1
Not AvailableCompletedTreatmentPregnancy1
Not AvailableCompletedTreatmentPremature Labour1

Pharmacoeconomics

Manufacturers
  • Abraxis pharmaceutical products
  • Hospira inc
  • Astrazeneca lp
Packagers
  • Solvay Pharmaceuticals
Dosage Forms
FormRouteStrength
Injection, solutionIntramuscular; Parenteral10 MG/2ML
Injection, solutionParenteral50 MG/5ML
TabletOral10 MG
InjectionIntramuscular; Intravenous
LiquidIntravenous10 mg / mL
TabletOral10 mg / tab
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)88-90 °CNot Available
water solubilityCompleteNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.179 mg/mLALOGPS
logP1.53ALOGPS
logP1.82Chemaxon
logS-3.2ALOGPS
pKa (Strongest Acidic)9.15Chemaxon
pKa (Strongest Basic)9.81Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count4Chemaxon
Polar Surface Area72.72 Å2Chemaxon
Rotatable Bond Count6Chemaxon
Refractivity83.02 m3·mol-1Chemaxon
Polarizability31.9 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9871
Blood Brain Barrier-0.8115
Caco-2 permeable-0.5546
P-glycoprotein substrateSubstrate0.692
P-glycoprotein inhibitor INon-inhibitor0.953
P-glycoprotein inhibitor IINon-inhibitor0.8732
Renal organic cation transporterNon-inhibitor0.6134
CYP450 2C9 substrateNon-substrate0.6367
CYP450 2D6 substrateSubstrate0.5054
CYP450 3A4 substrateNon-substrate0.5874
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9442
CYP450 2D6 inhibitorNon-inhibitor0.6034
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8351
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7277
Ames testNon AMES toxic0.7799
CarcinogenicityNon-carcinogens0.9177
BiodegradationNot ready biodegradable0.8862
Rat acute toxicity2.2303 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7534
hERG inhibition (predictor II)Inhibitor0.5409
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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Kind
Protein
Organism
Humans
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 ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
Molecular Weight
46458.32 Da
References
  1. Tanaka N, Tamai T, Mukaiyama H, Hirabayashi A, Muranaka H, Akahane S, Miyata H, Akahane M: Discovery of novel N-phenylglycine derivatives as potent and selective beta(3)-adrenoceptor agonists for the treatment of frequent urination and urinary incontinence. J Med Chem. 2001 Apr 26;44(9):1436-45. [Article]
  2. Schwarz MK, Page P: Preterm labour: an overview of current and emerging therapeutics. Curr Med Chem. 2003 Aug;10(15):1441-68. [Article]
  3. Lye SJ, Dayes BA, Freitag CL, Brooks J, Casper RF: Failure of ritodrine to prevent preterm labor in the sheep. Am J Obstet Gynecol. 1992 Nov;167(5):1399-408. [Article]
  4. Bianchetti A, Manara L: In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical beta-adrenoceptors in rat colon. Br J Pharmacol. 1990 Aug;100(4):831-9. [Article]
  5. Lenselink DR, Kuhlmann RS, Lawrence JM, Kolesari GL: Cardiovascular teratogenicity of terbutaline and ritodrine in the chick embryo. Am J Obstet Gynecol. 1994 Aug;171(2):501-6. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Basilisco G, Camboni MG, Bozzani A, Molgora M, Bianchi PA: Single doses of ritodrine delay orocaecal transit in patients with irritable bowel syndrome. Br J Clin Pharmacol. 1990 Mar;29(3):355-8. doi: 10.1111/j.1365-2125.1990.tb03647.x. [Article]
  8. Leveno KJ, Little BB, Cunningham FG: The national impact of ritodrine hydrochloride for inhibition of preterm labor. Obstet Gynecol. 1990 Jul;76(1):12-5. [Article]
  9. Fabry IG, De Paepe P, Kips JG, Van Bortel LM: The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels. Eur J Clin Pharmacol. 2011 Jun;67(6):573-80. doi: 10.1007/s00228-011-1040-5. Epub 2011 Apr 15. [Article]
  10. Shimokawa S, Sakata A, Suga Y, Isoda K, Itai S, Nagase K, Shimada T, Sai Y: Incidence and risk factors of neonatal hypoglycemia after ritodrine therapy in premature labor: a retrospective cohort study. J Pharm Health Care Sci. 2019 Apr 16;5:7. doi: 10.1186/s40780-019-0137-3. eCollection 2019. [Article]
  11. Brashear WT, Kuhnert BR, Wei R: Structural determination of the conjugated metabolites of ritodrine. Drug Metab Dispos. 1990 Jul-Aug;18(4):488-93. [Article]
  12. Fabry I, De Paepe P, Kips J, Vermeersch S, Van Bortel L: Different effects of tocolytic medication on blood pressure and blood pressure amplification. Eur J Clin Pharmacol. 2011 Jan;67(1):11-7. doi: 10.1007/s00228-010-0926-y. Epub 2010 Nov 16. [Article]
  13. Dennedy MC, Friel AM, Gardeil F, Morrison JJ: Beta-3 versus beta-2 adrenergic agonists and preterm labour: in vitro uterine relaxation effects. BJOG. 2001 Jun;108(6):605-9. doi: 10.1111/j.1471-0528.2001.00147.x. [Article]
  14. Brashear WT, Kuhnert BR, Wei R: Maternal and neonatal urinary excretion of sulfate and glucuronide ritodrine conjugates. Clin Pharmacol Ther. 1988 Dec;44(6):634-41. doi: 10.1038/clpt.1988.205. [Article]
  15. Pacifici GM, Quilici MC, Giulianetti B, Spisni R, Nervi M, Giuliani L, Gomeni R: Ritodrine sulphation in the human liver and duodenal mucosa: interindividual variability. Eur J Drug Metab Pharmacokinet. 1998 Jan-Mar;23(1):67-74. doi: 10.1007/BF03189829. [Article]
  16. Sato Y, Teraki Y, Izaki S, Baba K: Ritodrine-induced erythematous papular eruption in 14 pregnant women. Int J Dermatol. 2010 Dec;49(12):1450-3. doi: 10.1111/j.1365-4632.2010.04633.x. [Article]
  17. Wu CD, Chao AS, Cheng PJ, Soong YK: Ritodrine-induced leukopenia: a case report and literature review. Changgeng Yi Xue Za Zhi. 1996 Dec;19(4):388-91. [Article]
  18. Mangrella M, Torella M, Russo F, Rossi F, Piucci B, Cantoni V: [Pharmacology of ritodrine]. Minerva Ginecol. 1999 Jun;51(6):233-44. [Article]
  19. Chae J, Cho GJ, Oh MJ, Park K, Han SW, Choi SJ, Oh SY, Roh CR: In utero exposure to ritodrine during pregnancy and risk of autism in their offspring until 8 years of age. Sci Rep. 2021 Jan 13;11(1):1146. doi: 10.1038/s41598-020-80904-y. [Article]
  20. Pacifici GM, Kubrich M, Giuliani L, de Vries M, Rane A: Sulphation and glucuronidation of ritodrine in human foetal and adult tissues. Eur J Clin Pharmacol. 1993;44(3):259-64. doi: 10.1007/BF00271368. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Downregulator
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...

Components:
References
  1. Anumba DO, Ford GA, Boys RJ, Robson SC: Stimulated nitric oxide release and nitric oxide sensitivity in forearm arterial vasculature during normotensive and preeclamptic pregnancy. Am J Obstet Gynecol. 1999 Dec;181(6):1479-84. doi: 10.1016/s0002-9378(99)70394-7. [Article]
  2. Hamada Y, Nakaya Y, Hamada S, Kamada M, Aono T: Activation of K+ channels by ritodrine hydrochloride in uterine smooth muscle cells from pregnant women. Eur J Pharmacol. 1994 Dec 15;288(1):45-51. doi: 10.1016/0922-4106(94)90008-6. [Article]
  3. de Heus R, Mulder EJ, Derks JB, Visser GH: Acute tocolysis for uterine activity reduction in term labor: a review. Obstet Gynecol Surv. 2008 Jun;63(6):383-8; quiz 405. doi: 10.1097/OGX.0b013e31816ff75b. [Article]
  4. Caritis SN, Lin LS, Wong LK: Evaluation of the pharmacodynamics and pharmacokinetics of ritodrine when administered as a loading dose. On establishing a potentially useful drug administration regimen in cases of fetal distress. Am J Obstet Gynecol. 1985 Aug 15;152(8):1026-31. [Article]
  5. Ekblad U, Grenman S, Kaila T: The effect of a short-term ritodrine treatment on the concentration of beta-adrenergic receptors in human myometrium. Ann Chir Gynaecol Suppl. 1987;202:29-31. [Article]
  6. Pedzinska-Betiuk A, Modzelewska B, Jozwik M, Jozwik M, Kostrzewska A: Differences in the effects of beta2- and beta3-adrenoceptor agonists on spontaneous contractions of human nonpregnant myometrium. Ginekol Pol. 2011 Dec;82(12):918-24. [Article]
  7. Plenge-Tellechea F, Soler F, Fernandez-Belda F: Ritodrine inhibition of the plasma membrane Ca2+-ATPase from human erythrocyte. Arch Biochem Biophys. 1998 Sep 15;357(2):179-84. doi: 10.1006/abbi.1998.0812. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Activator
General Function
Phosphatidylinositol-4,5-bisphosphate binding
Specific Function
In the kidney, probably plays a major role in potassium homeostasis. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than...

Components:
References
  1. Hamada Y, Nakaya Y, Hamada S, Kamada M, Aono T: Activation of K+ channels by ritodrine hydrochloride in uterine smooth muscle cells from pregnant women. Eur J Pharmacol. 1994 Dec 15;288(1):45-51. doi: 10.1016/0922-4106(94)90008-6. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Signal transducer activity
Specific Function
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium.

Components:
References
  1. Plenge-Tellechea F, Soler F, Fernandez-Belda F: Ritodrine inhibition of the plasma membrane Ca2+-ATPase from human erythrocyte. Arch Biochem Biophys. 1998 Sep 15;357(2):179-84. doi: 10.1006/abbi.1998.0812. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Activator
General Function
Voltage-gated potassium channel activity
Specific Function
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activati...

Components:
References
  1. Hamada Y, Nakaya Y, Hamada S, Kamada M, Aono T: Activation of K+ channels by ritodrine hydrochloride in uterine smooth muscle cells from pregnant women. Eur J Pharmacol. 1994 Dec 15;288(1):45-51. doi: 10.1016/0922-4106(94)90008-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Calcium/calmodulin-dependent myosin light chain kinase implicated in smooth muscle contraction via phosphorylation of myosin light chains (MLC). Also regulates actin-myosin interaction through a non-kinase activity. Phosphorylates PTK2B/PYK2 and myosin light-chains. Involved in the inflammatory response (e.g. apoptosis, vascular permeability, leukocyte diapedesis), cell motility and morphology, airway hyperreactivity and other activities relevant to asthma. Required for tonic airway smooth muscle contraction that is necessary for physiological and asthmatic airway resistance. Necessary for gastrointestinal motility. Implicated in the regulation of endothelial as well as vascular permeability, probably via the regulation of cytoskeletal rearrangements. In the nervous system it has been shown to control the growth initiation of astrocytic processes in culture and to participate in transmitter release at synapses formed between cultured sympathetic ganglion cells. Critical participant in signaling sequences that result in fibroblast apoptosis. Plays a role in the regulation of epithelial cell survival. Required for epithelial wound healing, especially during actomyosin ring contraction during purse-string wound closure. Mediates RhoA-dependent membrane blebbing. Triggers TRPC5 channel activity in a calcium-dependent signaling, by inducing its subcellular localization at the plasma membrane. Promotes cell migration (including tumor cells) and tumor metastasis. PTK2B/PYK2 activation by phosphorylation mediates ITGB2 activation and is thus essential to trigger neutrophil transmigration during acute lung injury (ALI). May regulate optic nerve head astrocyte migration. Probably involved in mitotic cytoskeletal regulation. Regulates tight junction probably by modulating ZO-1 exchange in the perijunctional actomyosin ring. Mediates burn-induced microvascular barrier injury; triggers endothelial contraction in the development of microvascular hyperpermeability by phosphorylating MLC. Essential for intestinal barrier dysfunction. Mediates Giardia spp.-mediated reduced epithelial barrier function during giardiasis intestinal infection via reorganization of cytoskeletal F-actin and tight junctional ZO-1. Necessary for hypotonicity-induced Ca(2+) entry and subsequent activation of volume-sensitive organic osmolyte/anion channels (VSOAC) in cervical cancer cells. Responsible for high proliferative ability of breast cancer cells through anti-apoptosis.
Specific Function
Actin binding
Gene Name
MYLK
Uniprot ID
Q15746
Uniprot Name
Myosin light chain kinase, smooth muscle
Molecular Weight
210713.455 Da
References
  1. Sultatos LG: Mechanisms of drugs that affect uterine motility. J Nurse Midwifery. 1997 Jul-Aug;42(4):367-70. doi: 10.1016/s0091-2182(97)60134-2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of drugs, xenobiotic compounds, hormones, and neurotransmitters. May be involved in the activation of carcinogenic hydroxylamines. Shows activity towards p-nitrophenol and N-hydroxy-2-acetylamino-fluorene (N-OH-2AAF).
Specific Function
Aryl sulfotransferase activity
Gene Name
SULT1C4
Uniprot ID
O75897
Uniprot Name
Sulfotransferase 1C4
Molecular Weight
35519.635 Da
References
  1. Hui Y, Liu MC: Sulfation of ritodrine by the human cytosolic sulfotransferases (SULTs): Effects of SULT1A3 genetic polymorphism. Eur J Pharmacol. 2015 Aug 15;761:125-9. doi: 10.1016/j.ejphar.2015.04.039. Epub 2015 May 2. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phosphogluconate dehydrogenase (decarboxylating) activity
Specific Function
Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
Gene Name
PGD
Uniprot ID
P52209
Uniprot Name
6-phosphogluconate dehydrogenase, decarboxylating
Molecular Weight
53139.56 Da
References
  1. Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [Article]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of catecholamines, phenolic drugs and neurotransmitters. Has also estroge...
Gene Name
SULT1A1
Uniprot ID
P50225
Uniprot Name
Sulfotransferase 1A1
Molecular Weight
34165.13 Da
References
  1. Nishimuta H, Tsujimoto M, Ogura K, Hiratsuka A, Ohtani H, Sawada Y: Inhibitory effects of various beverages on ritodrine sulfation by recombinant human sulfotransferase isoforms SULT1A1 and SULT1A3. Pharm Res. 2005 Aug;22(8):1406-10. doi: 10.1007/s11095-005-5263-y. Epub 2005 Aug 3. [Article]
  2. Hui Y, Liu MC: Sulfation of ritodrine by the human cytosolic sulfotransferases (SULTs): Effects of SULT1A3 genetic polymorphism. Eur J Pharmacol. 2015 Aug 15;761:125-9. doi: 10.1016/j.ejphar.2015.04.039. Epub 2015 May 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs.
Specific Function
Amine sulfotransferase activity
Gene Name
SULT1A3
Uniprot ID
P0DMM9
Uniprot Name
Sulfotransferase 1A3
Molecular Weight
34195.96 Da
References
  1. Nishimuta H, Tsujimoto M, Ogura K, Hiratsuka A, Ohtani H, Sawada Y: Inhibitory effects of various beverages on ritodrine sulfation by recombinant human sulfotransferase isoforms SULT1A1 and SULT1A3. Pharm Res. 2005 Aug;22(8):1406-10. doi: 10.1007/s11095-005-5263-y. Epub 2005 Aug 3. [Article]
  2. Hui Y, Liu MC: Sulfation of ritodrine by the human cytosolic sulfotransferases (SULTs): Effects of SULT1A3 genetic polymorphism. Eur J Pharmacol. 2015 Aug 15;761:125-9. doi: 10.1016/j.ejphar.2015.04.039. Epub 2015 May 2. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.

Components:
References
  1. Hui Y, Liu MC: Sulfation of ritodrine by the human cytosolic sulfotransferases (SULTs): Effects of SULT1A3 genetic polymorphism. Eur J Pharmacol. 2015 Aug 15;761:125-9. doi: 10.1016/j.ejphar.2015.04.039. Epub 2015 May 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of drugs, xenobiotic compounds, hormones, and neurotransmitters. May be involved in the activation of carcinogenic hydroxylamines. Shows activity towards p-nitrophenol and N-hydroxy-2-acetylamino-fluorene (N-OH-2AAF).
Specific Function
Aryl sulfotransferase activity
Gene Name
SULT1C4
Uniprot ID
O75897
Uniprot Name
Sulfotransferase 1C4
Molecular Weight
35519.635 Da
References
  1. Hui Y, Liu MC: Sulfation of ritodrine by the human cytosolic sulfotransferases (SULTs): Effects of SULT1A3 genetic polymorphism. Eur J Pharmacol. 2015 Aug 15;761:125-9. doi: 10.1016/j.ejphar.2015.04.039. Epub 2015 May 2. [Article]

Drug created at June 13, 2005 13:24 / Updated at May 02, 2022 10:03