Misoprostol

Identification

Summary

Misoprostol is a prostaglandin E1 analogue used to reduce the risk of NSAID-induced gastric ulcers and to terminate pregnancies.

Brand Names
Arthrotec, Cytotec, Mifegymiso
Generic Name
Misoprostol
DrugBank Accession Number
DB00929
Background

Misoprostol is a prostaglandin analog used to reduce the risk of NSAID related ulcers, manage miscarriages, prevent post partum hemorrhage, and also for first trimester abortions.13,14,4,2,10 The stimulation of prostaglandin receptors in the stomach reduces gastric acid secretion, while stimulating these receptors in the uterus and cervix can increase the strength and frequency of contractions and decrease cervical tone.3

Misoprostol was granted FDA approval on 27 December 1988.13

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 382.5341
Monoisotopic: 382.271924326
Chemical Formula
C22H38O5
Synonyms
  • Misoprostol
  • Misoprostolum

Pharmacology

Indication

Misoprostol is indicated as a tablet to reduce the risk of NSAID induced gastric ulcers but not duodenal ulcers in high risk patients.13 Misoprostol is also formulated in combination with diclofenac to treat symptoms of osteoarthritis or rheumatoid arthritis in patients with a high risk of developing gastric ulcers.14 Misoprostol is used off label for the management of miscarriages, prevention of post partum hemorrhage, and is also used alone or in combination with mifepristone in other countries for first trimester abortions.4,2,10

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofGastric ulcer••••••••••••
Treatment ofIncomplete abortion••• •••••
Treatment ofMissed abortion••• •••••
Treatment ofPostpartum hemorrhage••• •••••
Prophylaxis ofPostpartum hemorrhage••• •••••
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Misoprostol is a prostaglandin E1 analog used to reduce the risk of NSAID induced gastric ulcers by reducing secretion of gastric acid from parietal cells.3,13,14 Misoprostol is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions.4,2,6 An oral dose of misoprostol has an 8 minute onset of action and a duration of action of approximately 2 hours, a sublingual dose has an 11 minute onset of action and a duration of action of approximately 3 hours, a vaginal dose has a 20 minute onset of action and a duration of action of approximately 4 hours, and a rectal dose has a 100 minute onset of action and a duration of action of approximately 4 hours.7

Mechanism of action

Misoprostol is a synthetic prostaglandin E1 analog that stimulates prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric acid secretion.3 Mucus and bicarbonate secretion are also increased along with thickening of the mucosal bilayer so the mucosa can generate new cells.3

Misoprostol binds to smooth muscle cells in the uterine lining to increase the strength and frequency of contractions as well as degrade collagen and reduce cervical tone.3

TargetActionsOrganism
AProstaglandin E2 receptor EP3 subtype
agonist
Humans
AProstaglandin E2 receptor EP2 subtype
agonist
Humans
AProstaglandin E2 receptor EP1 subtype
agonist
Humans
UProstaglandin E2 receptor EP4 subtype
agonist
Humans
Absorption

For an 800µg oral dose of misoprostol, the AUC was 2.0192±0.8032h*ng/mL, the Cmax was 2.6830±1.2161ng/mL, and a tmax of 0.345±0.186h.5 For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h*ng/mL, the Cmax was 2.4391±1.1567ng/mL, and a tmax of 0.712±0.415h.5 For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h*ng/mL, the Cmax was 1.3611±0.3436ng/mL, and a tmax of 1.308±0.624h.5

Volume of distribution

Data regarding the volume of distribution of misoprostol is scarce.

The apparent volume of distribution of the active metabolite of misoprostol was in subjects with normal renal function was 13.6±8.0L/kg, with mild renal impairment was 17.3±23.0L/kg, with moderate renal impairment was 14.3±6.8L/kg, and with end stage renal disease was 11.0±9.6L/kg.8

Protein binding

Misoprostol is <90% protein bound in serum.13,14 Its active metabolite, misoprostol acid, is 81-89% protein bound in serum.9

Metabolism

Misoprostol is de-esterified to its active metabolite, misoprostol acid, also known as SC-30695.1 This metabolite is further reduced to dinor and tetranor metabolites (SC-41411), a prostaglandin F1 (PGF1) analog of SC-41411, and a ω-16-carboxylic acid derivative.1 However, the majority of these metabolites are not well described in the literature.1

Hover over products below to view reaction partners

Route of elimination

As much as 73.2±4.6% of a radiolabelled oral dose of misoprostol is recovered in the urine.1,14

Half-life

The half life of an 800µg oral dose is 1.0401±0.5090h, for a sublingual dose is 0.8542±0.1170h, and for a buccal dose is 0.8365±0.1346h.5

Clearance

Because of the rapid de-esterification of misoprostol before or during absorption, it is usually undetectable in plasma.8 Misoprostol's active metabolite, misoprostol acid, has a total body clearance of 0.286L/kg/min.8 Subjects with mild renal impairment had a total body clearance of 0.226±0.073L/kg/min, subjects with moderate renal impairment had a total body clearance of 0.270±0.103L/kg/min, and subjects with end stage renal disease had a total body clearance of 0.105±0.052L/kg/min.8

Adverse Effects
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Toxicity

The oral LD50 in rats is 81mg/kg and in mice is 27mg/kg.12 The intraperitoneal LD50 in rats is 40mg/kg and in mice is 70mg/kg.12

Patients experiencing an overdose may present with sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea, fever, palpitations, hypotension, and bradycardia.11,13,14 Hemodialysis is not expected to be useful in the treatment of misoprostol overdose13 but oral activated charcoal may help reduce absorption.14 In the event of an overdose, treat symptoms with supportive therapy.13 This may include removal of undissolved tablets from the vagina or buccal cavity, intravenous fluid replacement, acetaminophen, diazepam, haloperidol, or intramuscular diclofenac depending on the symptoms that present.11

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
CarbetocinThe risk or severity of adverse effects can be increased when Misoprostol is combined with Carbetocin.
Carboprost tromethamineCarboprost tromethamine may increase the uterotonic activities of Misoprostol.
HydrotalciteThe risk or severity of adverse effects can be increased when Hydrotalcite is combined with Misoprostol.
MagaldrateThe risk or severity of adverse effects can be increased when Magaldrate is combined with Misoprostol.
MagnesiumThe risk or severity of adverse effects can be increased when Magnesium is combined with Misoprostol.
Food Interactions
  • Take with food. Food decreases incidence of diarrhea.

Products

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Product Images
International/Other Brands
Isprelor
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CytotecTablet100 ug/1OralPfizer Laboratories Div Pfizer Inc1986-12-27Not applicableUS flag
CytotecTablet200 ug/1OralA S Medication Solutions1986-12-27Not applicableUS flag
CytotecTablet100 ug/1OralPhysicians Total Care, Inc.1996-07-02Not applicableUS flag
CytotecTablet100 ug/1OralPD-Rx Pharmaceuticals, Inc.1986-12-27Not applicableUS flag
CytotecTablet200 ug/1OralCardinal Health1988-12-272015-12-31US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MisoprostolTablet200 ug/1OralNucare Pharmaceuticals,inc.2022-04-11Not applicableUS flag
MisoprostolTablet200 ug/1OralPharmacist Pharmaceutical, LLC2013-04-12Not applicableUS flag
MisoprostolTablet200 ug/1OralGenBioPro, Inc.2020-04-27Not applicableUS flag
MisoprostolTablet200 ug/1OralPD-Rx Pharmaceuticals, Inc.2022-04-11Not applicableUS flag
MisoprostolTablet200 ug/1OralGreenstone, Llc2009-12-27Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Act Diclo-misoMisoprostol (200 mcg) + Diclofenac sodium (75 mg)Tablet, delayed releaseOralActavis Pharma Company2013-03-272019-08-08Canada flag
Act Diclo-misoMisoprostol (200 mcg) + Diclofenac sodium (50 mg)Tablet, delayed releaseOralActavis Pharma Company2013-03-272019-08-08Canada flag
ArthrotecMisoprostol (200 ug/1) + Diclofenac sodium (50 mg/1)Tablet, film coatedOralPD-Rx Pharmaceuticals, Inc.1997-12-242019-09-12US flag
ArthrotecMisoprostol (200 ug/1) + Diclofenac sodium (75 mg/1)Tablet, film coatedOralbryant ranch prepack1997-12-242016-02-28US flag
ArthrotecMisoprostol (200 ug/1) + Diclofenac sodium (50 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2009-10-07Not applicableUS flag

Categories

ATC Codes
G02AD06 — MisoprostolA02BB01 — MisoprostolM01AE56 — Naproxen and misoprostol
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as prostaglandins and related compounds. These are unsaturated carboxylic acids consisting of a 20 carbon skeleton that also contains a five member ring, and are based upon the fatty acid arachidonic acid.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Fatty Acyls
Sub Class
Eicosanoids
Direct Parent
Prostaglandins and related compounds
Alternative Parents
Fatty acid methyl esters / Cyclopentanols / Tertiary alcohols / Methyl esters / Cyclic ketones / Cyclic alcohols and derivatives / Monocarboxylic acids and derivatives / Organic oxides / Hydrocarbon derivatives
Substituents
Alcohol / Aliphatic homomonocyclic compound / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Cyclic alcohol / Cyclic ketone / Cyclopentanol / Fatty acid ester / Fatty acid methyl ester
Molecular Framework
Aliphatic homomonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
0E43V0BB57
CAS number
59122-46-2
InChI Key
OJLOPKGSLYJEMD-URPKTTJQSA-N
InChI
InChI=1S/C22H38O5/c1-4-5-14-22(2,26)15-10-12-18-17(19(23)16-20(18)24)11-8-6-7-9-13-21(25)27-3/h10,12,17-18,20,24,26H,4-9,11,13-16H2,1-3H3/b12-10+/t17-,18-,20-,22?/m1/s1
IUPAC Name
methyl 7-[(1R,2R,3R)-3-hydroxy-2-[(1E)-4-hydroxy-4-methyloct-1-en-1-yl]-5-oxocyclopentyl]heptanoate
SMILES
CCCCC(C)(O)C\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC

References

Synthesis Reference

Salah Ahmed, Raj Mahajan, "Vaginal tablets comprising misoprostol and methods of making and using the same." U.S. Patent US20070071814, issued March 29, 2007.

US20070071814
General References
  1. Schoenhard G, Oppermann J, Kohn FE: Metabolism and pharmacokinetic studies of misoprostol. Dig Dis Sci. 1985 Nov;30(11 Suppl):126S-128S. doi: 10.1007/bf01309397. [Article]
  2. Turner JV, Agatonovic-Kustrn S, Ward H: Off-label use of misoprostol in gynaecology. Facts Views Vis Obgyn. 2015 Dec 28;7(4):261-264. [Article]
  3. Krugh M, Maani CV: Misoprostol . [Article]
  4. Speer L: Misoprostol Alone is Associated with High Rate of Successful First-Trimester Abortion. Am Fam Physician. 2019 Jul 15;100(2):119. [Article]
  5. Frye LJ, Byrne ME, Winikoff B: A crossover pharmacokinetic study of misoprostol by the oral, sublingual and buccal routes. Eur J Contracept Reprod Health Care. 2016 Aug;21(4):265-8. doi: 10.3109/13625187.2016.1168799. Epub 2016 Apr 22. [Article]
  6. Fjerstad M, Trussell J, Sivin I, Lichtenberg ES, Cullins V: Rates of serious infection after changes in regimens for medical abortion. N Engl J Med. 2009 Jul 9;361(2):145-51. doi: 10.1056/NEJMoa0809146. [Article]
  7. Tang OS, Gemzell-Danielsson K, Ho PC: Misoprostol: pharmacokinetic profiles, effects on the uterus and side-effects. Int J Gynaecol Obstet. 2007 Dec;99 Suppl 2:S160-7. doi: 10.1016/j.ijgo.2007.09.004. Epub 2007 Oct 26. [Article]
  8. Foote EF, Lee DR, Karim A, Keane WF, Halstenson CE: Disposition of misoprostol and its active metabolite in patients with normal and impaired renal function. J Clin Pharmacol. 1995 Apr;35(4):384-9. [Article]
  9. Cook CS, Schoenhard GL, Karim A: Effect of salicylic acid on the plasma protein binding and pharmacokinetics of misoprostol acid. J Pharm Sci. 1994 Jun;83(6):883-6. doi: 10.1002/jps.2600830625. [Article]
  10. Hobday K, Hulme J, Homer C, Zualo Wate P, Belton S, Prata N: "My job is to get pregnant women to the hospital": a qualitative study of the role of traditional birth attendants in the distribution of misoprostol to prevent post-partum haemorrhage in two provinces in Mozambique. Reprod Health. 2018 Oct 16;15(1):174. doi: 10.1186/s12978-018-0622-4. [Article]
  11. Barros JG, Reis I, Graca LM: Acute misoprostol toxicity during the first trimester of pregnancy. Int J Gynaecol Obstet. 2011 May;113(2):157-8. doi: 10.1016/j.ijgo.2010.12.006. Epub 2011 Feb 22. [Article]
  12. Cayman Chemicals: Misoprostol MSDS [Link]
  13. FDA Approved Drug Products: Misoprostol Tablets [Link]
  14. FDA Approved Drug Products: Misoprostol and Diclofenac Tablets [Link]
Human Metabolome Database
HMDB0015064
KEGG Drug
D00419
PubChem Compound
5282381
PubChem Substance
46505041
ChemSpider
4445541
BindingDB
85606
RxNav
42331
ChEBI
63610
ChEMBL
CHEMBL606
Therapeutic Targets Database
DAP000358
PharmGKB
PA450523
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Misoprostol
FDA label
Download (246 KB)
MSDS
Download (147 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentInduction of Labour1
4CompletedHealth Services ResearchAbortion, Therapeutic1
4CompletedHealth Services ResearchMenstrual Regulation1
4CompletedOtherContraceptive Device; Complications1
4CompletedPreventionBleeding During Myomectomy1

Pharmacoeconomics

Manufacturers
  • Gd searle llc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Packagers
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Chirogate International Inc.
  • Direct Dispensing Inc.
  • DispenseXpress Inc.
  • Dispensing Solutions
  • GD Searle LLC
  • Greenstone LLC
  • H.J. Harkins Co. Inc.
  • Hawkins Inc.
  • Innoviant Pharmacy Inc.
  • Ivax Pharmaceuticals
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
  • Physicians Total Care Inc.
  • Piramal Healthcare
  • Rebel Distributors Corp.
  • Southwood Pharmaceuticals
Dosage Forms
FormRouteStrength
Tablet25 MICROGRAMMI
TabletOral200.000 µg
Tablet, film coatedOral
Tablet, coatedOral
TabletOral
TabletOral0.200 mg
TabletVaginal25 mcg
TabletVaginal20000000 mg
TabletVaginal50 cg
Tablet, orally disintegratingOral400 mcg
TabletOral100 ug/1
TabletOral200 ug/1
TabletOral400 MCG
TabletOral200 mcg
TabletOral200 cg
Tablet, delayed releaseOral
TabletOral
TabletVaginal200 mcg
Tablet200 mg
TabletOral20.000 mg
Tablet
Kit; tabletBuccal; Oral
Tablet400 MICROGRAMMI
TabletOral100 mcg
Kit; tablet; tablet, orally disintegratingOral
Drug delivery systemVaginal200 mcg
TabletOral200.000 mcg
Tablet
Tablet200 mcg
Prices
Unit descriptionCostUnit
Misoprostol hpmc powder152.0USD g
Cytotec 60 200 mcg tablet Bottle121.93USD bottle
Cytotec 60 100 mcg tablet Bottle81.36USD bottle
Arthrotec 75 tablet ec4.07USD tablet
Arthrotec ec 50 mg-200 mcg tablet2.99USD tablet
Arthrotec ec 75 mg-200 mcg tablet2.99USD tablet
Arthrotec ec 75 tablet2.96USD tablet
Arthrotec 75 75-200 mg-mcg tablet2.82USD tablet
Arthrotec 50 50-200 mg-mcg tablet2.7USD tablet
Cytotec 200 mcg tablet1.95USD tablet
Cytotec 100 mcg tablet1.34USD tablet
Misoprostol 200 mcg tablet1.22USD tablet
Misoprostol 100 mcg tablet0.84USD tablet
Apo-Misoprostol 200 mcg Tablet0.45USD tablet
Apo-Misoprostol 100 mcg Tablet0.27USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5601843No1997-02-112014-02-11US flag
US5698225No1997-12-162010-05-03US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)261-263http://www.chemspider.com/Chemical-Structure.4445541.html
water solubility1.6mg/mLhttps://www.caymanchem.com/pdfs/13820.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0164 mg/mLALOGPS
logP3.88ALOGPS
logP3.86Chemaxon
logS-4.4ALOGPS
pKa (Strongest Acidic)14.69Chemaxon
pKa (Strongest Basic)-0.95Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area83.83 Å2Chemaxon
Rotatable Bond Count14Chemaxon
Refractivity107.88 m3·mol-1Chemaxon
Polarizability45.44 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9157
Blood Brain Barrier+0.938
Caco-2 permeable-0.5339
P-glycoprotein substrateSubstrate0.6607
P-glycoprotein inhibitor INon-inhibitor0.7261
P-glycoprotein inhibitor IIInhibitor0.6504
Renal organic cation transporterNon-inhibitor0.9146
CYP450 2C9 substrateNon-substrate0.857
CYP450 2D6 substrateNon-substrate0.9024
CYP450 3A4 substrateSubstrate0.6281
CYP450 1A2 substrateNon-inhibitor0.8358
CYP450 2C9 inhibitorNon-inhibitor0.8175
CYP450 2D6 inhibitorNon-inhibitor0.9459
CYP450 2C19 inhibitorNon-inhibitor0.8199
CYP450 3A4 inhibitorNon-inhibitor0.795
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9591
Ames testNon AMES toxic0.8289
CarcinogenicityNon-carcinogens0.8941
BiodegradationNot ready biodegradable0.8797
Rat acute toxicity3.7051 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.964
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0zgl-7669000000-5ba5f8c705e7fe123902
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0029000000-f3907635f7331ff3eb6d
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-03e9-0009000000-7a97814b180ef54d1e90
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001j-0019000000-2547611a647bfe53f4ce
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-052b-4696000000-e0130b98821e7e20c1be
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0zi0-6279000000-dc8948fc7abb81fa3f3a
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0pe9-2910000000-cdd65ac8b750de4866e2
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-212.8705905
predicted
DarkChem Lite v0.1.0
[M-H]-227.9700905
predicted
DarkChem Lite v0.1.0
[M-H]-207.58379
predicted
DeepCCS 1.0 (2019)
[M+H]+214.5217905
predicted
DarkChem Lite v0.1.0
[M+H]+230.7699905
predicted
DarkChem Lite v0.1.0
[M+H]+209.942
predicted
DeepCCS 1.0 (2019)
[M+Na]+212.1805905
predicted
DarkChem Lite v0.1.0
[M+Na]+216.19978
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Rna polymerase ii transcription factor activity, ligand-activated sequence-specific dna binding
Specific Function
Receptor for prostaglandin E2 (PGE2); the EP3 receptor may be involved in inhibition of gastric acid secretion, modulation of neurotransmitter release in central and peripheral neurons, inhibition ...
Gene Name
PTGER3
Uniprot ID
P43115
Uniprot Name
Prostaglandin E2 receptor EP3 subtype
Molecular Weight
43309.335 Da
References
  1. Nakae K, Hayashi F, Hayashi M, Yamamoto N, Iino T, Yoshikawa S, Gupta J: Functional role of prostacyclin receptor in rat dorsal root ganglion neurons. Neurosci Lett. 2005 Nov 18;388(3):132-7. [Article]
  2. Li J, Liang X, Wang Q, Breyer RM, McCullough L, Andreasson K: Misoprostol, an anti-ulcer agent and PGE2 receptor agonist, protects against cerebral ischemia. Neurosci Lett. 2008 Jun 20;438(2):210-5. doi: 10.1016/j.neulet.2008.04.054. Epub 2008 Apr 20. [Article]
  3. Guan Y, Stillman BA, Zhang Y, Schneider A, Saito O, Davis LS, Redha R, Breyer RM, Breyer MD: Cloning and expression of the rabbit prostaglandin EP2 receptor. BMC Pharmacol. 2002 Jun 27;2:14. [Article]
  4. Kiriyama M, Ushikubi F, Kobayashi T, Hirata M, Sugimoto Y, Narumiya S: Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. [Article]
  5. Nataraj C, Thomas DW, Tilley SL, Nguyen MT, Mannon R, Koller BH, Coffman TM: Receptors for prostaglandin E(2) that regulate cellular immune responses in the mouse. J Clin Invest. 2001 Oct;108(8):1229-35. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Prostaglandin e receptor activity
Specific Function
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. The subsequent raise in intracellular cAMP is responsible for the ...
Gene Name
PTGER2
Uniprot ID
P43116
Uniprot Name
Prostaglandin E2 receptor EP2 subtype
Molecular Weight
39759.945 Da
References
  1. Nakae K, Hayashi F, Hayashi M, Yamamoto N, Iino T, Yoshikawa S, Gupta J: Functional role of prostacyclin receptor in rat dorsal root ganglion neurons. Neurosci Lett. 2005 Nov 18;388(3):132-7. [Article]
  2. Li J, Liang X, Wang Q, Breyer RM, McCullough L, Andreasson K: Misoprostol, an anti-ulcer agent and PGE2 receptor agonist, protects against cerebral ischemia. Neurosci Lett. 2008 Jun 20;438(2):210-5. doi: 10.1016/j.neulet.2008.04.054. Epub 2008 Apr 20. [Article]
  3. Guan Y, Stillman BA, Zhang Y, Schneider A, Saito O, Davis LS, Redha R, Breyer RM, Breyer MD: Cloning and expression of the rabbit prostaglandin EP2 receptor. BMC Pharmacol. 2002 Jun 27;2:14. [Article]
  4. Kiriyama M, Ushikubi F, Kobayashi T, Hirata M, Sugimoto Y, Narumiya S: Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. [Article]
  5. Nataraj C, Thomas DW, Tilley SL, Nguyen MT, Mannon R, Koller BH, Coffman TM: Receptors for prostaglandin E(2) that regulate cellular immune responses in the mouse. J Clin Invest. 2001 Oct;108(8):1229-35. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Prostaglandin e receptor activity
Specific Function
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an importa...
Gene Name
PTGER1
Uniprot ID
P34995
Uniprot Name
Prostaglandin E2 receptor EP1 subtype
Molecular Weight
41800.655 Da
References
  1. Krugh M, Maani CV: Misoprostol . [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Prostaglandin e receptor activity
Specific Function
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role...
Gene Name
PTGER4
Uniprot ID
P35408
Uniprot Name
Prostaglandin E2 receptor EP4 subtype
Molecular Weight
53118.845 Da
References
  1. Nakae K, Hayashi F, Hayashi M, Yamamoto N, Iino T, Yoshikawa S, Gupta J: Functional role of prostacyclin receptor in rat dorsal root ganglion neurons. Neurosci Lett. 2005 Nov 18;388(3):132-7. [Article]
  2. Li J, Liang X, Wang Q, Breyer RM, McCullough L, Andreasson K: Misoprostol, an anti-ulcer agent and PGE2 receptor agonist, protects against cerebral ischemia. Neurosci Lett. 2008 Jun 20;438(2):210-5. doi: 10.1016/j.neulet.2008.04.054. Epub 2008 Apr 20. [Article]
  3. Guan Y, Stillman BA, Zhang Y, Schneider A, Saito O, Davis LS, Redha R, Breyer RM, Breyer MD: Cloning and expression of the rabbit prostaglandin EP2 receptor. BMC Pharmacol. 2002 Jun 27;2:14. [Article]
  4. Kiriyama M, Ushikubi F, Kobayashi T, Hirata M, Sugimoto Y, Narumiya S: Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. [Article]
  5. Nataraj C, Thomas DW, Tilley SL, Nguyen MT, Mannon R, Koller BH, Coffman TM: Receptors for prostaglandin E(2) that regulate cellular immune responses in the mouse. J Clin Invest. 2001 Oct;108(8):1229-35. [Article]
  6. Crider JY, Xu SX, Sharif NA: Pharmacology of functional endogenous IP prostanoid receptors in NCB-20 cells: comparison with binding data from human platelets. Prostaglandins Leukot Essent Fatty Acids. 2001 Nov-Dec;65(5-6):253-8. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48