Ritodrine

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

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Ritodrine (DB00867)

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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

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Pharmacology

Indication

For the treatment and prophylaxis of premature labour

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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		••••••••••••		•• ••••••••••••••••• •• •••••••••	•••••••••

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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.

Target	Actions	Organism
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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Integrate drug-drug interactions in your software
Acebutolol	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.

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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
Yutopar Tab 10mg	Tablet	10 mg / tab	Oral	Bristol Labs Division Of Bristol Myers Squibb	1984-12-31	2001-07-30

Categories

ATC Codes

G02CA01 — Ritodrine

• G02CA — Sympathomimetics, labour repressants
• G02C — OTHER GYNECOLOGICALS
• G02 — OTHER GYNECOLOGICALS
• G — GENITO URINARY SYSTEM AND SEX HORMONES

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

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Prevention	Premature Births	1
4	Unknown Status	Prevention	Preterm Labor Without Delivery	1
1	Completed	Treatment	Healthy Subjects (HS)	1
Not Available	Completed	Treatment	Pregnancy	1
Not Available	Completed	Treatment	Premature Labour	1

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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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Details1. Beta-2 adrenergic receptor

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]

Details2. Beta adrenergic receptor (Protein Group)

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...

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Components:

Name	UniProt ID
Beta-1 adrenergic receptor	P08588
Beta-2 adrenergic receptor	P07550
Beta-3 adrenergic receptor	P13945

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]

Details3. ATP-sensitive potassium channel (Protein Group)

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...

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Components:

Name	UniProt ID
ATP-sensitive inward rectifier potassium channel 1	P48048
ATP-sensitive inward rectifier potassium channel 10	P78508
ATP-sensitive inward rectifier potassium channel 11	Q14654
ATP-sensitive inward rectifier potassium channel 12	Q14500
ATP-sensitive inward rectifier potassium channel 14	Q9UNX9
ATP-sensitive inward rectifier potassium channel 15	Q99712
ATP-sensitive inward rectifier potassium channel 8	Q15842

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]

Details4. Calcium transporting ATPases (Protein Group)

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:

Name	UniProt ID
Calcium-transporting ATPase type 2C member 1	P98194
Calcium-transporting ATPase type 2C member 2	O75185
Plasma membrane calcium-transporting ATPase 1	P20020
Plasma membrane calcium-transporting ATPase 2	Q01814
Plasma membrane calcium-transporting ATPase 3	Q16720
Plasma membrane calcium-transporting ATPase 4	P23634
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1	O14983
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2	P16615

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]

Details5. Calcium-activated potassium channel (Protein Group)

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...

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Components:

Name	UniProt ID
Calcium-activated potassium channel subunit alpha-1	Q12791
Calcium-activated potassium channel subunit beta-1	Q16558
Calcium-activated potassium channel subunit beta-2	Q9Y691
Calcium-activated potassium channel subunit beta-3	Q9NPA1
Calcium-activated potassium channel subunit beta-4	Q86W47
Intermediate conductance calcium-activated potassium channel protein 4	O15554
Small conductance calcium-activated potassium channel protein 1	Q92952
Small conductance calcium-activated potassium channel protein 2	Q9H2S1
Small conductance calcium-activated potassium channel protein 3	Q9UGI6

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]

Details6. Myosin light chain kinase, smooth muscle

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]

Details7. Sulfotransferase 1C4

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]

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Drug created at June 13, 2005 13:24 / Updated at February 02, 2024 22:45