Explore a selection of our essential drug information below, or:
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
Structure for Ritodrine (DB00867)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Foetal distress syndrome •••••••••••• ••••••••• Prevention of Premature births •••••••••••• ••••••••• Prevention of Premature births •••••••••••• ••••••••• Treatment of Premature labour •••••••••••• •• ••••••••••••••••• •• ••••••••• ••••••••• Prevention of Uterine contractions •••••••••••• •• ••••••••••••••••• •• ••••••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism ABeta-2 adrenergic receptor agonistHumans ABeta adrenergic receptor agonistdownregulatorHumans AATP-sensitive potassium channel activatorHumans ACalcium-activated potassium channel activatorHumans UCalcium transporting ATPases inhibitorHumans UMyosin light chain kinase, smooth muscle inhibitorHumans USulfotransferase 1C4 substrateHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol The therapeutic efficacy of Ritodrine can be decreased when used in combination with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Ritodrine is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Ritodrine is combined with Acemetacin. Acetylsalicylic acid The risk or severity of hypertension can be increased when Ritodrine is combined with Acetylsalicylic acid. Aclidinium The risk or severity of Tachycardia can be increased when Ritodrine is combined with Aclidinium. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Ritodrine hydrochloride ESJ56Q60GC 23239-51-2 IDLSITKDRVDKRV-JSUROZADSA-N - International/Other Brands
- Yutopar
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Yutopar Inj 50mg/5ml Liquid 10 mg / mL Intravenous Bristol Labs Division Of Bristol Myers Squibb 1984-12-31 2001-07-30 Canada 
Yutopar Tab 10mg Tablet 10 mg / tab Oral Bristol Labs Division Of Bristol Myers Squibb 1984-12-31 2001-07-30 Canada
Categories
- ATC Codes
- G02CA01 — Ritodrine
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic beta-2 Receptor Agonists
- Adrenergic beta-Agonists
- Agents producing tachycardia
- Agents that produce hypertension
- Alcohols
- Amines
- Amino Alcohols
- Autonomic Agents
- Ethylamines
- Genito Urinary System and Sex Hormones
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Phenethylamines
- Propanolamines
- Propanols
- Reproductive Control Agents
- Sympathomimetics
- Sympathomimetics, Labour Repressants
- Tocolytic Agents
- 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
- External Links
- Human Metabolome Database
- HMDB0015005
- KEGG Drug
- D02359
- KEGG Compound
- C07239
- PubChem Compound
- 33572
- PubChem Substance
- 46505273
- ChemSpider
- 599993
- BindingDB
- 50493311
- 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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Treatment Pregnancy 1 somestatus stop reason just information to hide Not Available Completed Treatment Premature Labour 1 somestatus stop reason just information to hide 4 Completed Prevention Premature Births 1 somestatus stop reason just information to hide 4 Unknown Status Prevention Preterm Labor Without Delivery 1 somestatus stop reason just information to hide 1 Completed Treatment Healthy Volunteers (HV) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Abraxis pharmaceutical products
- Hospira inc
- Astrazeneca lp
- Packagers
- Solvay Pharmaceuticals
- Dosage Forms
Form Route Strength Injection, solution Intramuscular; Parenteral 10 MG/2ML Injection, solution Parenteral 50 MG/5ML Tablet Oral 10 MG Injection Intramuscular; Intravenous 50 mg/5ml Liquid Intravenous 10 mg / mL Tablet Oral 10 mg / tab - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 88-90 °C Not Available water solubility Complete Not Available logP 2.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.179 mg/mL ALOGPS logP 1.53 ALOGPS logP 1.82 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 9.15 Chemaxon pKa (Strongest Basic) 9.81 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 72.72 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 83.02 m3·mol-1 Chemaxon Polarizability 31.9 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9871 Blood Brain Barrier - 0.8115 Caco-2 permeable - 0.5546 P-glycoprotein substrate Substrate 0.692 P-glycoprotein inhibitor I Non-inhibitor 0.953 P-glycoprotein inhibitor II Non-inhibitor 0.8732 Renal organic cation transporter Non-inhibitor 0.6134 CYP450 2C9 substrate Non-substrate 0.6367 CYP450 2D6 substrate Substrate 0.5054 CYP450 3A4 substrate Non-substrate 0.5874 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9442 CYP450 2D6 inhibitor Non-inhibitor 0.6034 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8351 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7277 Ames test Non AMES toxic 0.7799 Carcinogenicity Non-carcinogens 0.9177 Biodegradation Not ready biodegradable 0.8862 Rat acute toxicity 2.2303 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7534 hERG inhibition (predictor II) Inhibitor 0.5409
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-00di-0390000000-abbd425d79d56a23ea26 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0390000000-ad8ef1967e65dc65cf51 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0h90-1930000000-ad77657291c4c06be656 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0930000000-a0242608e80f564502ba Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0076-6910000000-bfcca5e46d2bd87266b0 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0zmi-1910000000-8f8c61c0ebd6bafd1620 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine
- Specific Function
- adenylate cyclase binding
- Gene Name
- ADRB2
- Uniprot ID
- P07550
- Uniprot Name
- Beta-2 adrenergic receptor
- Molecular Weight
- 46458.32 Da
References
- 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]
- Schwarz MK, Page P: Preterm labour: an overview of current and emerging therapeutics. Curr Med Chem. 2003 Aug;10(15):1441-68. [Article]
- 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]
- 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]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Mangrella M, Torella M, Russo F, Rossi F, Piucci B, Cantoni V: [Pharmacology of ritodrine]. Minerva Ginecol. 1999 Jun;51(6):233-44. [Article]
- 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]
- 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
- AgonistDownregulator
- General 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 equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling. Involved in the regulation of sleep/wake behaviors (PubMed:31473062)
- Specific Function
- alpha-2A adrenergic receptor binding
Components:
| Name | UniProt ID |
|---|---|
| Beta-1 adrenergic receptor | P08588 |
| Beta-2 adrenergic receptor | P07550 |
| Beta-3 adrenergic receptor | P13945 |
References
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- 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 out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. This channel is activated by internal ATP and can be blocked by external barium
- Specific Function
- ATP binding
Components:
References
- 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
- Yes
- Actions
- Activator
- General Function
- Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+) (PubMed:14523450, PubMed:29330545, PubMed:31152168). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX)
- Specific Function
- actin binding
Components:
References
- 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
- ATP-driven pump that supplies the Golgi apparatus with Ca(2+) and Mn(2+) ions, both essential cofactors for processing and trafficking of newly synthesized proteins in the secretory pathway (PubMed:12707275, PubMed:16192278, PubMed:20439740, PubMed:21187401, PubMed:30923126). Within a catalytic cycle, acquires Ca(2+) or Mn(2+) ions on the cytoplasmic side of the membrane and delivers them to the lumenal side. The transfer of ions across the membrane is coupled to ATP hydrolysis and is associated with a transient phosphorylation that shifts the pump conformation from inward-facing to outward-facing state (PubMed:16192278, PubMed:16332677, PubMed:30923126). Plays a primary role in the maintenance of Ca(2+) homeostasis in the trans-Golgi compartment with a functional impact on Golgi and post-Golgi protein sorting as well as a structural impact on cisternae morphology (PubMed:14632183, PubMed:20439740). Responsible for loading the Golgi stores with Ca(2+) ions in keratinocytes, contributing to keratinocyte differentiation and epidermis integrity (PubMed:10615129, PubMed:14632183, PubMed:20439740). Participates in Ca(2+) and Mn(2+) ions uptake into the Golgi store of hippocampal neurons and regulates protein trafficking required for neural polarity (By similarity). May also play a role in the maintenance of Ca(2+) and Mn(2+) homeostasis and signaling in the cytosol while preventing cytotoxicity (PubMed:21187401)
- Specific Function
- ATP binding
Components:
References
- 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
- 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
- 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 phenolic compounds. Can also sulfonate estrogenic compounds, however, the dietary flavonoids (phytoestrogen) and environmental estrogens, like bisphenol A are better substrates than 17beta-estradiol (E2) (PubMed:17425406, PubMed:26948952, PubMed:28222028, PubMed:9852044). Mediates the sulfation of doxorubicin and its analog epirubicin, two antitumor anthracyclines (PubMed:26948952)
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1C4
- Uniprot ID
- O75897
- Uniprot Name
- Sulfotransferase 1C4
- Molecular Weight
- 35519.635 Da
References
- 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
- Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH
- Specific Function
- NADP binding
- Gene Name
- PGD
- Uniprot ID
- P52209
- Uniprot Name
- 6-phosphogluconate dehydrogenase, decarboxylating
- Molecular Weight
- 53139.56 Da
References
- 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]
- 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 that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of a wide variety of acceptor molecules bearing a hydroxyl or an amine groupe. Sulfonation increases the water solubility of most compounds, and therefore their renal excretion, but it can also result in bioactivation to form active metabolites. Displays broad substrate specificity for small phenolic compounds. Plays an important role in the sulfonation of endogenous molecules such as steroid hormones and 3,3'-diiodothyronin (PubMed:10199779, PubMed:12471039, PubMed:16221673, PubMed:21723874, PubMed:22069470, PubMed:7834621). Mediates the sulfate conjugation of a variety of xenobiotics, including the drugs acetaminophen and minoxidil (By similarity). Mediates also the metabolic activation of carcinogenic N-hydroxyarylamines leading to highly reactive intermediates capable of forming DNA adducts, potentially resulting in mutagenesis (PubMed:7834621). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system
- Specific Function
- 3'-phosphoadenosine 5'-phosphosulfate binding
- Gene Name
- SULT1A1
- Uniprot ID
- P50225
- Uniprot Name
- Sulfotransferase 1A1
- Molecular Weight
- 34165.13 Da
References
- 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]
- 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
- 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]
- 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 that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of a wide variety of acceptor molecules bearing a hydroxyl or an amine groupe. Sulfonation increases the water solubility of most compounds, and therefore their renal excretion, but it can also result in bioactivation to form active metabolites. Displays broad substrate specificity for small phenolic compounds. Plays an important role in the sulfonation of endogenous molecules such as steroid hormones and 3,3'-diiodothyronin (PubMed:10199779, PubMed:12471039, PubMed:16221673, PubMed:21723874, PubMed:22069470, PubMed:7834621). Mediates the sulfate conjugation of a variety of xenobiotics, including the drugs acetaminophen and minoxidil (By similarity). Mediates also the metabolic activation of carcinogenic N-hydroxyarylamines leading to highly reactive intermediates capable of forming DNA adducts, potentially resulting in mutagenesis (PubMed:7834621). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system
- Specific Function
- 3'-phosphoadenosine 5'-phosphosulfate binding
Components:
References
- 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 compounds. Can also sulfonate estrogenic compounds, however, the dietary flavonoids (phytoestrogen) and environmental estrogens, like bisphenol A are better substrates than 17beta-estradiol (E2) (PubMed:17425406, PubMed:26948952, PubMed:28222028, PubMed:9852044). Mediates the sulfation of doxorubicin and its analog epirubicin, two antitumor anthracyclines (PubMed:26948952)
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1C4
- Uniprot ID
- O75897
- Uniprot Name
- Sulfotransferase 1C4
- Molecular Weight
- 35519.635 Da
References
- 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 October 03, 2024 07:07