NAV

Misoprostol

Identification

Summary

Misoprostolis 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.13,14,4,2,10The 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
 3D
Similar Structures
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.13Misoprostol 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.14Misoprostol 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
Associated Therapies
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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.3,13,14Misoprostol is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions.4,2,6An 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.3Mucus 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

Target Actions Organism
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 Cmaxwas 2.6830±1.2161ng/mL, and a tmaxof 0.345±0.186h.5For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h*ng/mL, the Cmaxwas 2.4391±1.1567ng/mL, and a tmaxof 0.712±0.415h.5For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h*ng/mL, the Cmaxwas 1.3611±0.3436ng/mL, and a tmaxof 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.13,14Its 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-30695.1This 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.1However, the majority of these metabolites are not well described in the literature.1

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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.8Misoprostol's active metabolite, misoprostol acid, has a total body clearance of 0.286L/kg/min.8科目有轻度肾功能损害总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 LD50in rats is 81mg/kg and in mice is 27mg/kg.12The intraperitoneal LD50in 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.11,13,14Hemodialysis is not expected to be useful in the treatment of misoprostol overdose13but oral activated charcoal may help reduce absorption.14In the event of an overdose, treat symptoms with supportive therapy.13This 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
不可用
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Interactions

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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
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interactions in your software
Carbetocin The risk or severity of adverse effects can be increased when Misoprostol is combined with Carbetocin.
Carboprost tromethamine Carboprost tromethamine may increase the uterotonic activities of Misoprostol.
Hydrotalcite The risk or severity of adverse effects can be increased when Hydrotalcite is combined with Misoprostol.
Magaldrate The risk or severity of adverse effects can be increased when Magaldrate is combined with Misoprostol.
Magnesium The risk or severity of adverse effects can be increased when Magnesium is combined with Misoprostol.
Magnesium carbonate The risk or severity of adverse effects can be increased when Magnesium carbonate is combined with Misoprostol.
Magnesium chloride The risk or severity of adverse effects can be increased when Magnesium chloride is combined with Misoprostol.
Magnesium citrate The risk or severity of adverse effects can be increased when Magnesium citrate is combined with Misoprostol.
Magnesium gluconate The risk or severity of adverse effects can be increased when Magnesium gluconate is combined with Misoprostol.
Magnesium hydroxide The risk or severity of adverse effects can be increased when Magnesium hydroxide is combined with Misoprostol.
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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
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Cytotec Tablet 200 ug/1 Oral A S Medication Solutions 1986-12-27 不适用 US flag
Cytotec Tablet 100 ug/1 Oral Physicians Total Care, Inc. 1996-07-02 不适用 US flag
Cytotec Tablet 100 ug/1 Oral PD-Rx Pharmaceuticals, Inc. 1986-12-27 不适用 US flag
Cytotec Tablet 200 ug/1 Oral Cardinal Health 1988-12-27 2015-12-31 US flag
Cytotec Tablet 200 ug/1 Oral Apotheca, Inc. 2010-01-01 不适用 US flag
Cytotec Tablet 200 ug/1 Oral Pfizer Laboratories Div Pfizer Inc 1986-12-27 不适用 US flag
Cytotec Tablet 100 ug/1 Oral Cardinal Health 1988-12-27 2015-12-31 US flag
Cytotec Tablet 100 ug/1 Oral Pfizer Laboratories Div Pfizer Inc 1986-12-27 不适用 US flag
Cytotec 100 Mcg Tablet 100 mcg Oral Pfizer Canada Ulc 1989-12-31 2004-07-26 Canada flag
Cytotec 200 Mcg Tablet 200 mcg Oral Pfizer Canada Ulc 1986-12-31 2005-08-05 Canada flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Misoprostol Tablet 100 ug/1 Oral bryant ranch prepack 2012-07-25 不适用 US flag
Misoprostol Tablet 200 ug/1 Oral GenBioPro, Inc. 2009-12-27 不适用 US flag
Misoprostol Tablet 200 ug/1 Oral American Health Packaging 2023-04-01 不适用 US flag
Misoprostol Tablet 200 ug/1 Oral Ready Meds 2012-07-25 不适用 US flag
Misoprostol Tablet 200 ug/1 Oral KAISER FOUNDATION HOSPITALS 2016-09-20 2019-12-31 US flag
Misoprostol Tablet 200 ug/1 Oral Cadila Healthcare Limited 2020-01-14 不适用 US flag
Misoprostol Tablet 100 ug/1 Oral bryant ranch prepack 2009-12-27 不适用 US flag
Misoprostol Tablet 100 ug/1 Oral IVAX Pharmaceuticals, Inc. 2002-07-10 2013-10-31 US flag
Misoprostol Tablet 200 ug/1 Oral Novel Laboratories, Inc. 2012-07-25 不适用 US flag
Misoprostol Tablet 100 ug/1 Oral Major Pharmaceuticals 2012-07-25 不适用 US flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Act Diclo-miso Misoprostol(200 mcg)+Diclofenac sodium(75 mg) Tablet, delayed release Oral Actavis Pharma Company 2013-03-27 2019-08-08 Canada flag
Act Diclo-miso Misoprostol(200 mcg)+Diclofenac sodium(50 mg) Tablet, delayed release Oral Actavis Pharma Company 2013-03-27 2019-08-08 Canada flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral bryant ranch prepack 1997-12-24 2016-02-28 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral Pfizer Laboratories Div Pfizer Inc 1997-12-24 不适用 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(50 mg/1) Tablet, film coated Oral Physicians Total Care, Inc. 2009-10-07 不适用 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral A-S Medication Solutions 1997-12-24 不适用 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral Lake Erie Medical & Surgical Supply DBA Quality Care Products LLC 2012-02-23 2019-10-11 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral Stat Rx USA 1997-12-24 不适用 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(50 mg/1) Tablet, film coated Oral Pfizer Laboratories Div Pfizer Inc 1997-12-24 不适用 US flag
Arthrotec Misoprostol(200 ug/1)+Diclofenac sodium(75 mg/1) Tablet, film coated Oral Rebel Distributors 1997-12-24 不适用 US flag

Categories

ATC Codes
G02AD06 — Misoprostol A02BB01 — Misoprostol M01AE56 — Naproxen and misoprostol
Drug Categories
Chemical TaxonomyProvided byClassyfire
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
不可用
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
一般引用
  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
药物.com
药物.com Drug Page
Wikipedia
Misoprostol
FDA label
Download (246 KB)
MSDS
Download (147 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions 数
4 Active Not Recruiting Other Menstrual Irregularities/Menstrual Regulation 1
4 Active Not Recruiting Prevention Blood Loss During Surgery/Intrapartum Hemorrhage 1
4 Completed Health Services Research Abortion, Therapeutic 1
4 Completed Health Services Research Menstrual Regulation 1
4 Completed Other Contraceptive Device; Complications 1
4 Completed Prevention Bleeding During Myomectomy 1
4 Completed Prevention Hemorrhage 1
4 Completed Prevention Intra-uterine Device Complication 1
4 Completed Prevention NSAID-associated Gastroduodenal Injury 1
4 Completed Prevention Placenta Previa 1

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塞尔有限责任公司
  • 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
Form Route Strength
Tablet 25 MICROGRAMMI
Tablet, film coated Oral
Tablet, coated Oral
Tablet Oral
Tablet Vaginal 25 mcg
Tablet Vaginal 200 mg
Tablet Vaginal 50 cg
Tablet, orally disintegrating Oral 400 mcg
Tablet Oral 100 ug/1
Tablet Oral 200 ug/1
Tablet Oral 400 MCG
Tablet Oral 200 mcg
Tablet Oral 200 cg
Tablet, delayed release Oral
Tablet Oral
Tablet Vaginal 200 mcg
Tablet 200 mg
Tablet
Kit; tablet Buccal; Oral
Tablet 400 MICROGRAMMI
Tablet Oral 100 mcg
Drug delivery system Vaginal 200 mcg
Tablet
Tablet 200 mcg
Prices
Unit description Cost Unit
Misoprostol hpmc powder 152.0USD g
Cytotec 60 200 mcg tablet Bottle 121.93USD bottle
Cytotec 60 100 mcg tablet Bottle 81.36USD bottle
Arthrotec 75 tablet ec 4.07USD tablet
Arthrotec ec 50 mg-200 mcg tablet 2.99USD tablet
Arthrotec ec 75 mg-200 mcg tablet 2.99USD tablet
Arthrotec ec 75 tablet 2.96USD tablet
Arthrotec 75 75-200 mg-mcg tablet 2.82USD tablet
Arthrotec 50 50-200 mg-mcg tablet 2.7USD tablet
Cytotec 200 mcg tablet 1.95USD tablet
Cytotec 100 mcg tablet 1.34USD tablet
Misoprostol 200 mcg tablet 1.22USD tablet
Misoprostol 100 mcg tablet 0.84USD tablet
Apo-Misoprostol 200 mcg Tablet 0.45USD tablet
Apo-Misoprostol 100 mcg Tablet 0.27USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region
US5601843 No 1997-02-11 2014-02-11 US flag
US5698225 No 1997-12-16 2010-05-03 US flag

Properties

State
Liquid
Experimental Properties
Property Value Source
melting point (°C) 261-263 http://www.chemspider.com/Chemical-Structure.4445541.html
water solubility 1.6mg/mL https://www.caymanchem.com/pdfs/13820.pdf
Predicted Properties
Property Value Source
Water Solubility 0.0164 mg/mL ALOGPS
logP 3.88 ALOGPS
logP 3.86 Chemaxon
logS -4.4 ALOGPS
pKa (Strongest Acidic) 14.69 Chemaxon
pKa (Strongest Basic) -0.95 Chemaxon
Physiological Charge 0 Chemaxon
Hydrogen Acceptor Count 4 Chemaxon
Hydrogen Donor Count 2 Chemaxon
Polar Surface Area 83.83 Å2 Chemaxon
Rotatable Bond Count 14 Chemaxon
Refractivity 107.88 m3·mol-1 Chemaxon
Polarizability 45.44 Å3 Chemaxon
Number of Rings 1 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five Yes Chemaxon
Ghose Filter Yes Chemaxon
Veber's Rule No Chemaxon
MDDR-like规则 No Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9157
Blood Brain Barrier + 0.938
Caco-2 permeable - 0.5339
P-glycoprotein substrate Substrate 0.6607
P-glycoprotein inhibitor I Non-inhibitor 0.7261
P-glycoprotein inhibitor II Inhibitor 0.6504
Renal organic cation transporter Non-inhibitor 0.9146
CYP450 2C9 substrate Non-substrate 0.857
CYP450 2D6 substrate Non-substrate 0.9024
CYP450 3A4 substrate Substrate 0.6281
CYP450 1A2 substrate Non-inhibitor 0.8358
CYP450 2C9 inhibitor Non-inhibitor 0.8175
CYP450 2D6 inhibitor Non-inhibitor 0.9459
CYP450 2C19 inhibitor Non-inhibitor 0.8199
CYP450 3A4 inhibitor Non-inhibitor 0.795
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9591
Ames test Non AMES toxic 0.8289
Carcinogenicity Non-carcinogens 0.8941
Biodegradation Not ready biodegradable 0.8797
Rat acute toxicity 3.7051 LD50, mol/kg 不适用
hERG inhibition (predictor I) Weak inhibitor 0.964
hERG inhibition (predictor II) Non-inhibitor 0.8734
ADMET data is predicted usingadmetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
不可用
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS 不可用
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS 不可用

Targets

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insights and accelerate drug research.
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Details 1.Prostaglandin E2 receptor EP3 subtype
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
分子量
43309.335 Da
References
  1. 山本Nakae K, Hayashi F, Hayashi M, 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]
Details 2.Prostaglandin E2 receptor EP2 subtype
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
分子量
39759.945 Da
References
  1. 山本Nakae K, Hayashi F, Hayashi M, 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]
Details 3.Prostaglandin E2 receptor EP1 subtype
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
分子量
41800.655 Da
References
  1. Krugh M, Maani CV: Misoprostol . [Article]
Details 4.Prostaglandin E2 receptor EP4 subtype
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
分子量
53118.845 Da
References
  1. 山本Nakae K, Hayashi F, Hayashi M, 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司法院,徐SX,谢里夫NA:药理功能ional 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 April 11, 2023 21:34