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References

Trials

Economics

Properties

Spectra

Taxonomy

Dinoprostone

Targets (5)Enzymes (3)Transporters (17)Biointeractions (28)

Identification

Name

Dinoprostone

Accession Number

DB00917 (APRD00927)

Type

Small Molecule

Groups

Approved

Description

Dinoprostone is a naturally occurring prostaglandin E2 (PGE2). It has important effects in labour. It also stimulates osteoblasts to release factors which stimualtes bone resorption by osteoclasts. As a prescription drug it is used as a vaginal suppository, to prepare the cervix for labour and to induce labour.

Structure

Similar Structures

Synonyms

(15S)-Prostaglandin e2
(5Z,11alpha,13e,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dien-1-oic acid
(5Z,13e)-(15S)-11alpha,15-Dihydroxy-9-oxoprost-13-enoate
(5Z,13e)-(15S)-11alpha,15-Dihydroxy-9-oxoprosta-5,13-dienoate
(e,Z)-(1R,2R,3R)-7-(3-Hydroxy-2-((3S)-(3-hydroxy-1-octenyl))-5-oxocyclopentyl)-5-heptenoic acid
(Z)-7-((1R,2R,3R)-3-Hydroxy-2-((S,e)-3-hydroxyoct-1-enyl)-5-oxocyclopentyl)hept-5-enoic acid
Dinoproston
Dinoprostona
Dinoprostone
Dinoprostone Prostaglandin E2
Dinoprostonum
PGE2
Propess
Prostaglandin E2

External IDs

U-12,062 / U-12062

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Cervidil	Insert	10 mg/241mg	Vaginal	Ferring Pharmaceuticals	1995-03-30	Not applicable
Cervidil	Insert	10 mg	Vaginal	Ferring Pharmaceuticals	1997-06-17	Not applicable
Cervidil	Insert, extended release	10 mg/1	Vaginal	Forest Laboratories	1995-05-19	2015-12-31
Dinoprostone	Insert	10 mg/241mg	Vaginal	Ferring Pharmaceuticals	2014-02-01	Not applicable
Prepidil	Gel	0.5 mg/3g	Vaginal	Pharmacia & Upjohn Inc	1992-12-09	Not applicable
Prepidil Gel	Gel	0.5 mg	Endocervical	Pfizer	1990-12-31	Not applicable
Prostin E2	Suppository	20 mg/1	Vaginal	Pharmacia & Upjohn Inc	1978-01-18	Not applicable
Prostin E2 Tablets	Tablet	0.5 mg	Oral	Pfizer	1977-12-31	Not applicable
Prostin E2 Vaginal Gel	Gel	2 mg	Vaginal	Pfizer	1991-12-31	Not applicable
Prostin E2 Vaginal Gel	Gel	1 mg	Vaginal	Pfizer	1991-12-31	Not applicable

International/Other Brands

Prepidil / Propess (Ferring Pharmaceuticals) / Prostarmon E (DCPC) / PROSTIN / Prostin e2

Categories

UNII

K7Q1JQR04M

CAS number

363-24-6

Weight

Average: 352.4651
Monoisotopic: 352.224974134

Chemical Formula

C₂₀H₃₂O₅

InChI Key

XEYBRNLFEZDVAW-ARSRFYASSA-N

InChI

InChI=1S/C20H32O5/c1-2-3-6-9-15(21)12-13-17-16(18(22)14-19(17)23)10-7-4-5-8-11-20(24)25/h4,7,12-13,15-17,19,21,23H,2-3,5-6,8-11,14H2,1H3,(H,24,25)/b7-4-,13-12+/t15-,16+,17+,19+/m0/s1

IUPAC Name

(5Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]hept-5-enoic acid

SMILES

CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O

Pharmacology

Indication

For the termination of pregnancy during the second trimester (from the 12th through the 20th gestational week as calculated from the first day of the last normal menstrual period), as well as for evacuation of the uterine contents in the management of missed abortion or intrauterine fetal death up to 28 weeks of gestational age as calculated from the first day of the last normal menstrual period. Also used in the management of nonmetastatic gestational trophoblastic disease (benign hydatidiform mole). Other indications include improving the cervical inducibility (cervical "ripening") in pregnant women at or near term with a medical or obstetrical need for labor induction, and the management of postpartum hemorrhage.

Associated Conditions

Gestational Trophoblastic Disease

Associated Therapies

Pharmacodynamics

Dinoprostone is equivalent to prostaglandin E2 (PGE2). It stimulates labor and delivery by stimulating the uterine, and thus terminates pregnancy. Dinoprostone is also capable of stimulating the smooth muscle of the gastrointestinal tract of man. This activity may be responsible for the vomiting and/or diarrhea that is not uncommon when dinoprostone is used to terminate pregnancy.

Mechanism of action

Dinoprostone administered intravaginally stimulates the myometrium of the gravid uterus to contract in a manner that is similar to the contractions seen in the term uterus during labor, resulting in the evacuation of the products of conception from the uterus. It is believed that dinoprostone exerts its uterine effects via direct myometrial stimulation, but the exact mechanism of action is unkown. Other suggested mechanisms include the regulation of cellular membrane calcium transport and of intracellular concentrations of cyclic 3',5'-adenosine monophosphate. Dinoprostone also appears to produce local cervical effects including softening, effacement, and dilation. The exact mechanism of action for this effect is also unknown, but it has been suggested that this effect may be associated with collagen degradation caused by secretion of the enzyme collagenase as a partial response to locally administered dinoprostone.

Target	Actions	Organism
AProstaglandin E2 receptor EP2 subtype	agonist	Human
AProstaglandin E2 receptor EP1 subtype	agonist	Human
AProstaglandin E2 receptor EP3 subtype	agonist	Human
AProstaglandin E2 receptor EP4 subtype	agonist	Human
UProstaglandin D2 receptor 2	agonist	Human

Absorption

Absorbed at a rate of 0.3 mg per hour over 12 hours while the vaginal system is in place.

Volume of distribution

Not Available

Protein binding

73%, to albumin

Metabolism

Rapid metabolism of dinoprostone occurs primarily in the local tissues; any systemic absorption of the medication is cleared mainly in the maternal lungs and, secondarily, at sites such as the liver and kidneys.

Route of elimination

The major route of elimination of the products of PGE2 metabolism is the kidneys.

Half life

Less than 5 minutes.

Clearance

Not Available

Toxicity

Oral, mouse: LD₅₀ = 750 mg/kg; Oral, rat: LD₅₀ = 500 mg/kg.

Affected organisms

Humans and other mammals

Pathways

Pathway	Category
Etodolac Action Pathway	Drug action
Ibuprofen Action Pathway	Drug action
Mefenamic Acid Action Pathway	Drug action
Carprofen Action Pathway	Drug action
Tiaprofenic Acid Action Pathway	Drug action
Diclofenac Action Pathway	Drug action
Indomethacin Action Pathway	Drug action
Meloxicam Action Pathway	Drug action
Nabumetone Action Pathway	Drug action
Naproxen Action Pathway	Drug action
Etoricoxib Action Pathway	Drug action
Arachidonic Acid Metabolism	Metabolic
Piroxicam Action Pathway	Drug action
Sulindac Action Pathway	Drug action
Celecoxib Action Pathway	Drug action
Bromfenac Action Pathway	Drug action
Antrafenine Action Pathway	Drug action
Magnesium Salicylate Action Pathway	Drug action
Lornoxicam Action Pathway	Drug action
Acetaminophen Action Pathway	Drug action
Oxaprozin Action Pathway	Drug action
Diflunisal Action Pathway	Drug action
Antipyrine Action Pathway	Drug action
Fenoprofen Action Pathway	Drug action
Flurbiprofen Action Pathway	Drug action
Phenylbutazone Action Pathway	Drug action
Nepafenac Action Pathway	Drug action
Tenoxicam Action Pathway	Drug action
Salicylic Acid Action Pathway	Drug action
Arachidonic Acid Metabolism	Metabolic

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction
3-isobutyl-1-methyl-7H-xanthine	The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Dinoprostone.
6-O-benzylguanine	The serum concentration of 6-O-benzylguanine can be increased when it is combined with Dinoprostone.
7-Deazaguanine	The serum concentration of 7-Deazaguanine can be increased when it is combined with Dinoprostone.
7,9-Dimethylguanine	The serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Dinoprostone.
8-azaguanine	The serum concentration of 8-azaguanine can be increased when it is combined with Dinoprostone.
8-chlorotheophylline	The serum concentration of 8-chlorotheophylline can be increased when it is combined with Dinoprostone.
9-Deazaguanine	The serum concentration of 9-Deazaguanine can be increased when it is combined with Dinoprostone.
9-Methylguanine	The serum concentration of 9-Methylguanine can be increased when it is combined with Dinoprostone.
Abiraterone	The serum concentration of Dinoprostone can be increased when it is combined with Abiraterone.
Aceclofenac	The therapeutic efficacy of Dinoprostone can be decreased when used in combination with Aceclofenac.

Food Interactions

Not Available

References

Synthesis Reference

Yu-Wen Su, Meng-Hwan Lee, "Composition for inhibiting nitric oxide and/or prostaglandin E2 synthesis and method for inhibiting inflammation." U.S. Patent US20080268078, issued October 30, 2008.

US20080268078

General References

Not Available

External Links

Human Metabolome Database: HMDB0001220
KEGG Drug: D00079
KEGG Compound: C00584
PubChem Compound: 5280360
PubChem Substance: 46505549
ChemSpider: 4444059
BindingDB: 35847
ChEBI: 15551
ChEMBL: CHEMBL548
Therapeutic Targets Database: DAP000360
PharmGKB: PA449345
IUPHAR: 1916
Guide to Pharmacology: GtP Drug Page
HET: P2E
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Dinoprostone

ATC Codes

G02AD02 — Dinoprostone

AHFS Codes

76:00.00 — Oxytocics

PDB Entries

3wfh

MSDS

Download (69.1 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1, 2	Unknown Status	Treatment	Fetal Demise / Fetal Membranes, Premature Rupture / Preeclampsia	1
2	Completed	Treatment	Delivery Uterine	1
2	Completed	Treatment	Early Amniotomy, Unfavorable Cervix	1
2	Completed	Treatment	Unfavorable Cervix, Cervical Ripening	1
2	Recruiting	Not Available	Induction of Labour	1
2	Recruiting	Treatment	Induction of Labour	1
2	Recruiting	Treatment	Induction of Uterine contractions	1
2, 3	Completed	Treatment	Induction of Labor Affected Fetus / Newborn	1
3	Completed	Not Available	Induction / Labour / PROM (Pregnancy)	1
3	Completed	Treatment	Cervical Ripening	1
3	Completed	Treatment	Cervical Ripening / Induction of Labour	2
3	Completed	Treatment	Cervical Ripening / Induction of Labour / Reducing Time to Vaginal Delivery	1
3	Completed	Treatment	Induction of Labour	1
3	Completed	Treatment	Labour Pain	1
3	Completed	Treatment	Pregnancy	1
3	Recruiting	Treatment	Cervical Ripening	1
3	Recruiting	Treatment	Cervical Ripening / Pregnancy	1
3	Recruiting	Treatment	Induction of Labor Affected Fetus / Newborn	1
3	Unknown Status	Treatment	Medical Induction of Labor Affecting Fetus	1
4	Completed	Not Available	Intrapartum Fetal Monitoring / Pregnancy	1
4	Completed	Treatment	Cervical Ripening / Induction of Labour	1
4	Completed	Treatment	Pregnancy	1
4	Completed	Treatment	Premature Rupture of Membranes at Term	2
4	Not Yet Recruiting	Treatment	Premature Rupture of Fetal Membranes	1
4	Recruiting	Health Services Research	Childbirth Problems / Labor Complications	1
4	Recruiting	Treatment	Cervical Ripening / Induction of Labour	1
4	Recruiting	Treatment	Induction of Labour	1
4	Recruiting	Treatment	PROM (Premature Rupture Of Foetal Membrane)	1
4	Terminated	Treatment	Cesarean Section / Vaginal Delivery	1
4	Unknown Status	Treatment	Cervical Ripening	1
Not Available	Active Not Recruiting	Treatment	Cervical Ripening / Induction of Labour	1
Not Available	Completed	Not Available	"Migraine-like" Headache / Migraine-like Headache	1
Not Available	Completed	Not Available	Headaches / Migraines	1
Not Available	Completed	Screening	Other Diseases or Conditions	1
Not Available	Completed	Treatment	BMI >30 kg/m2 / Induction of Labour / Pregnancy	1
Not Available	Completed	Treatment	Cervical Ripening / Induction of Uterine contractions	1
Not Available	Completed	Treatment	Failed Labour	1
Not Available	Completed	Treatment	Induction of Uterine contractions	1
Not Available	Enrolling by Invitation	Other	Cervical Ripening / Labour; Induced / Pilot Study	1
Not Available	Not Yet Recruiting	Treatment	Cesarean Section; Dehiscence / Labor Complications / Pregnancy Related	1
Not Available	Not Yet Recruiting	Treatment	Failed Medical or Unspecified Induction of Labor	1
Not Available	Recruiting	Treatment	Failed Induction of Labor	3
Not Available	Recruiting	Treatment	Induction of Labour	1
Not Available	Recruiting	Treatment	Medical Induction of Labor Affecting Newborn	1
Not Available	Recruiting	Treatment	Nulliparous Women Who Scheduled for Labor Induction	1
Not Available	Terminated	Treatment	Delivery	1
Not Available	Unknown Status	Not Available	Induction of Uterine contractions	1

Pharmacoeconomics

Manufacturers

Pharmacia and upjohn co
Controlled therapeutics (scotland) ltd

Packagers

Controlled Therapeutics Ltd.
Forest Pharmaceuticals
Pfizer Inc.
Pharmacia Inc.

Dosage forms

Form	Route	Strength
Insert	Vaginal	10 mg
Insert, extended release	Vaginal	10 mg/1
Insert	Vaginal	10 mg/241mg
Gel	Vaginal	0.5 mg/3g
Gel	Endocervical	0.5 mg
Suppository	Vaginal	20 mg/1
Tablet	Oral	0.5 mg
Gel	Vaginal	1 mg
Gel	Vaginal	2 mg

Prices

Unit description	Cost	Unit
Prostin e2 vaginal 20 mg sup	1177.04USD	each
Cervidil 10 mg vaginal insrt	256.13USD	each
Prepidil 0.5 mg/3 gm gel	104.94USD	g

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5269321	No	1995-07-14	2012-07-14

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	67 °C	PhysProp
water solubility	58.1 mg/L	Not Available
logP	2.82	HANSCH,C ET AL. (1995)

Predicted Properties

Property	Value	Source
Water Solubility	0.044 mg/mL	ALOGPS
logP	3.31	ALOGPS
logP	3.23	ChemAxon
logS	-3.9	ALOGPS
pKa (Strongest Acidic)	4.3	ChemAxon
pKa (Strongest Basic)	-1.6	ChemAxon
Physiological Charge	-1	ChemAxon
Hydrogen Acceptor Count	5	ChemAxon
Hydrogen Donor Count	3	ChemAxon
Polar Surface Area	94.83 Å²	ChemAxon
Rotatable Bond Count	12	ChemAxon
Refractivity	99.44 m³·mol^-1	ChemAxon
Polarizability	41 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 Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9815
Blood Brain Barrier	+	0.8704
Caco-2 permeable	+	0.5245
P-glycoprotein substrate	Substrate	0.5554
P-glycoprotein inhibitor I	Non-inhibitor	0.9202
P-glycoprotein inhibitor II	Non-inhibitor	0.8983
Renal organic cation transporter	Non-inhibitor	0.9064
CYP450 2C9 substrate	Non-substrate	0.8211
CYP450 2D6 substrate	Non-substrate	0.8834
CYP450 3A4 substrate	Non-substrate	0.5292
CYP450 1A2 substrate	Non-inhibitor	0.9045
CYP450 2C9 inhibitor	Non-inhibitor	0.9502
CYP450 2D6 inhibitor	Non-inhibitor	0.9231
CYP450 2C19 inhibitor	Non-inhibitor	0.9025
CYP450 3A4 inhibitor	Non-inhibitor	0.8309
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9725
Ames test	Non AMES toxic	0.9387
Carcinogenicity	Non-carcinogens	0.9201
Biodegradation	Ready biodegradable	0.6056
Rat acute toxicity	2.9631 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9087
hERG inhibition (predictor II)	Non-inhibitor	0.9138

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
GC-MS Spectrum - GC-MS (1 MEOX; 3 TMS)	GC-MS	splash10-0059-4920000000-6108934d406ea4062761
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
GC-MS Spectrum - GC-MS	GC-MS	splash10-0059-4920000000-6108934d406ea4062761
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 20V, Negative	LC-MS/MS	splash10-00yi-0398000000-41c3a62b076046d87381
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 25V, Negative	LC-MS/MS	splash10-00di-0495000000-df406a9e4cc995523a7e
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 30V, Negative	LC-MS/MS	splash10-00dr-0592000000-928e66269ab2854faa42
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 35V, Negative	LC-MS/MS	splash10-00dr-0590000000-b364a55fc0598d9265b5
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 40V, Negative	LC-MS/MS	splash10-00dr-0890000000-b3a25d975f2a38d7e49f
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 45V, Negative	LC-MS/MS	splash10-0079-0960000000-c67461d3bd965cbf289c
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 50V, Negative	LC-MS/MS	splash10-000i-0920000000-830ad149a4fe8f36e211
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 55V, Negative	LC-MS/MS	splash10-07br-0910000000-35e5bd204c947e2c4bcc
LC-MS/MS Spectrum - LC-ESI-QIT (4000Q TRAP, Applied Biosystems) 60V, Negative	LC-MS/MS	splash10-05fs-0900000000-573b0c5a4593210b387a
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-00yi-0398000000-612bce8f105beae0c5f2
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-00di-0495000000-78584a9b664c5155b473
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-00dr-0592000000-b37d658cf7b0d590aad4
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-00dr-0590000000-985f93ab468aa6a8a1b8
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-00dr-0890000000-5757ca5e8720a47086dc
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-0079-0960000000-c67461d3bd965cbf289c
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-000i-0920000000-830ad149a4fe8f36e211
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-07br-0910000000-35e5bd204c947e2c4bcc
LC-MS/MS Spectrum - LC-ESI-QIT , negative	LC-MS/MS	splash10-05fs-0900000000-573b0c5a4593210b387a
LC-MS/MS Spectrum - LC-ESI-QQ , negative	LC-MS/MS	splash10-00di-0294000000-9d89acbe9e631d718a4b
LC-MS/MS Spectrum - LC-ESI-QQ , negative	LC-MS/MS	splash10-00or-0096000000-67e3460a07ad1397b529
1H NMR Spectrum	1D NMR	Not Applicable
[1H,13C] 2D NMR Spectrum	2D NMR	Not Applicable

Taxonomy

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: Long-chain fatty acids / Hydroxy fatty acids / Unsaturated fatty acids / Cyclopentanols / Cyclic ketones / Cyclic alcohols and derivatives / Monocarboxylic acids and derivatives / Carboxylic acids / Organic oxides / Hydrocarbon derivatives
Substituents: Prostaglandin skeleton / Long-chain fatty acid / Hydroxy fatty acid / Cyclopentanol / Fatty acid / Unsaturated fatty acid / Cyclic alcohol / Ketone / Cyclic ketone / Secondary alcohol
Molecular Framework: Aliphatic homomonocyclic compounds
External Descriptors: prostaglandins E (CHEBI:15551) / Prostaglandins (C00584) / Prostaglandins (LMFA03010003)

Targets

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	37.7	N/A	N/A	20218623
Ki (nM)	4.9	N/A	N/A	10634944 / 17531488 / 17931866 / 18039575

Details1. Prostaglandin E2 receptor EP2 subtype

Kind: Protein
Organism: Human
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

Baryawno N, Sveinbjornsson B, Eksborg S, Orrego A, Segerstrom L, Oqvist CO, Holm S, Gustavsson B, Kagedal B, Kogner P, Johnsen JI: Tumor-growth-promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets. Neuro Oncol. 2008 Oct;10(5):661-74. doi: 10.1215/15228517-2008-035. Epub 2008 Aug 20. [PubMed:18715952]
Tamiji J, Crawford DA: Prostaglandin E(2) and misoprostol induce neurite retraction in Neuro-2a cells. Biochem Biophys Res Commun. 2010 Jul 30;398(3):450-6. doi: 10.1016/j.bbrc.2010.06.098. Epub 2010 Jun 27. [PubMed:20599704]
Legler DF, Bruckner M, Uetz-von Allmen E, Krause P: Prostaglandin E2 at new glance: novel insights in functional diversity offer therapeutic chances. Int J Biochem Cell Biol. 2010 Feb;42(2):198-201. doi: 10.1016/j.biocel.2009.09.015. Epub 2009 Sep 27. [PubMed:19788928]
Sugimoto Y, Narumiya S: Prostaglandin E receptors. J Biol Chem. 2007 Apr 20;282(16):11613-7. Epub 2007 Feb 28. [PubMed:17329241]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	1.1	N/A	N/A	20218623
Ki (nM)	9.1	N/A	N/A	17531488 / 18039575

Details2. Prostaglandin E2 receptor EP1 subtype

Kind: Protein
Organism: Human
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

Baryawno N, Sveinbjornsson B, Eksborg S, Orrego A, Segerstrom L, Oqvist CO, Holm S, Gustavsson B, Kagedal B, Kogner P, Johnsen JI: Tumor-growth-promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets. Neuro Oncol. 2008 Oct;10(5):661-74. doi: 10.1215/15228517-2008-035. Epub 2008 Aug 20. [PubMed:18715952]
Tamiji J, Crawford DA: Prostaglandin E(2) and misoprostol induce neurite retraction in Neuro-2a cells. Biochem Biophys Res Commun. 2010 Jul 30;398(3):450-6. doi: 10.1016/j.bbrc.2010.06.098. Epub 2010 Jun 27. [PubMed:20599704]
Legler DF, Bruckner M, Uetz-von Allmen E, Krause P: Prostaglandin E2 at new glance: novel insights in functional diversity offer therapeutic chances. Int J Biochem Cell Biol. 2010 Feb;42(2):198-201. doi: 10.1016/j.biocel.2009.09.015. Epub 2009 Sep 27. [PubMed:19788928]
Sugimoto Y, Narumiya S: Prostaglandin E receptors. J Biol Chem. 2007 Apr 20;282(16):11613-7. Epub 2007 Feb 28. [PubMed:17329241]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	0.94	N/A	N/A	20218623
Ki (nM)	0.33	N/A	N/A	17531488 / 18039575

Details3. Prostaglandin E2 receptor EP3 subtype

Kind: Protein
Organism: Human
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

Baryawno N, Sveinbjornsson B, Eksborg S, Orrego A, Segerstrom L, Oqvist CO, Holm S, Gustavsson B, Kagedal B, Kogner P, Johnsen JI: Tumor-growth-promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets. Neuro Oncol. 2008 Oct;10(5):661-74. doi: 10.1215/15228517-2008-035. Epub 2008 Aug 20. [PubMed:18715952]
Tamiji J, Crawford DA: Prostaglandin E(2) and misoprostol induce neurite retraction in Neuro-2a cells. Biochem Biophys Res Commun. 2010 Jul 30;398(3):450-6. doi: 10.1016/j.bbrc.2010.06.098. Epub 2010 Jun 27. [PubMed:20599704]
Legler DF, Bruckner M, Uetz-von Allmen E, Krause P: Prostaglandin E2 at new glance: novel insights in functional diversity offer therapeutic chances. Int J Biochem Cell Biol. 2010 Feb;42(2):198-201. doi: 10.1016/j.biocel.2009.09.015. Epub 2009 Sep 27. [PubMed:19788928]
Sugimoto Y, Narumiya S: Prostaglandin E receptors. J Biol Chem. 2007 Apr 20;282(16):11613-7. Epub 2007 Feb 28. [PubMed:17329241]

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	3	N/A	N/A	12643927 / 18039575
IC 50 (nM)	0.7	N/A	N/A	12643927
IC 50 (nM)	9.9	N/A	N/A	20218623
Ki (nM)	0.79	N/A	N/A	17531488 / 17931866 / 18039575

Details4. Prostaglandin E2 receptor EP4 subtype

Kind: Protein
Organism: Human
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. 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

Wise H: Lack of interaction between prostaglandin E2 receptor subtypes in regulating adenylyl cyclase activity in cultured rat dorsal root ganglion cells. Eur J Pharmacol. 2006 Mar 27;535(1-3):69-77. Epub 2006 Mar 20. [PubMed:16545798]
Baryawno N, Sveinbjornsson B, Eksborg S, Orrego A, Segerstrom L, Oqvist CO, Holm S, Gustavsson B, Kagedal B, Kogner P, Johnsen JI: Tumor-growth-promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets. Neuro Oncol. 2008 Oct;10(5):661-74. doi: 10.1215/15228517-2008-035. Epub 2008 Aug 20. [PubMed:18715952]
Tamiji J, Crawford DA: Prostaglandin E(2) and misoprostol induce neurite retraction in Neuro-2a cells. Biochem Biophys Res Commun. 2010 Jul 30;398(3):450-6. doi: 10.1016/j.bbrc.2010.06.098. Epub 2010 Jun 27. [PubMed:20599704]
Legler DF, Bruckner M, Uetz-von Allmen E, Krause P: Prostaglandin E2 at new glance: novel insights in functional diversity offer therapeutic chances. Int J Biochem Cell Biol. 2010 Feb;42(2):198-201. doi: 10.1016/j.biocel.2009.09.015. Epub 2009 Sep 27. [PubMed:19788928]
Sugimoto Y, Narumiya S: Prostaglandin E receptors. J Biol Chem. 2007 Apr 20;282(16):11613-7. Epub 2007 Feb 28. [PubMed:17329241]

Details5. Prostaglandin D2 receptor 2

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Agonist

General Function: Prostaglandin j receptor activity
Specific Function: Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is al...
Gene Name: PTGDR2
Uniprot ID: Q9Y5Y4
Uniprot Name: Prostaglandin D2 receptor 2
Molecular Weight: 43267.15 Da

References

Wright DH, Metters KM, Abramovitz M, Ford-Hutchinson AW: Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist. Br J Pharmacol. 1998 Apr;123(7):1317-24. [PubMed:9579725]

Enzymes

Details1. Cholesterol side-chain cleavage enzyme, mitochondrial

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, nad(p)h as one donor, and incorporation of one atom of oxygen
Specific Function: Catalyzes the side-chain cleavage reaction of cholesterol to pregnenolone.
Gene Name: CYP11A1
Uniprot ID: P05108
Uniprot Name: Cholesterol side-chain cleavage enzyme, mitochondrial
Molecular Weight: 60101.87 Da

References

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Details2. Cytochrome P450 19A1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inducer

General Function: Oxygen binding
Specific Function: Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name: CYP19A1
Uniprot ID: P11511
Uniprot Name: Aromatase
Molecular Weight: 57882.48 Da

References

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Details3. Cytochrome P450 1A2

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP1A2
Uniprot ID: P05177
Uniprot Name: Cytochrome P450 1A2
Molecular Weight: 58293.76 Da

References

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Details1. Solute carrier family 22 member 2

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Quaternary ammonium group transmembrane transporter activity
Specific Function: Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name: SLC22A2
Uniprot ID: O15244
Uniprot Name: Solute carrier family 22 member 2
Molecular Weight: 62579.99 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]

Details2. Solute carrier family 22 member 1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Secondary active organic cation transmembrane transporter activity
Specific Function: Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name: SLC22A1
Uniprot ID: O15245
Uniprot Name: Solute carrier family 22 member 1
Molecular Weight: 61153.345 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]

Details3. Multidrug resistance-associated protein 5

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Organic anion transmembrane transporter activity
Specific Function: Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name: ABCC5
Uniprot ID: O15440
Uniprot Name: Multidrug resistance-associated protein 5
Molecular Weight: 160658.8 Da

References

Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. [PubMed:12835412]

Details4. Solute carrier family 22 member 6

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name: SLC22A6
Uniprot ID: Q4U2R8
Uniprot Name: Solute carrier family 22 member 6
Molecular Weight: 61815.78 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]
Lu R, Chan BS, Schuster VL: Cloning of the human kidney PAH transporter: narrow substrate specificity and regulation by protein kinase C. Am J Physiol. 1999 Feb;276(2 Pt 2):F295-303. [PubMed:9950961]
Sekine T, Watanabe N, Hosoyamada M, Kanai Y, Endou H: Expression cloning and characterization of a novel multispecific organic anion transporter. J Biol Chem. 1997 Jul 25;272(30):18526-9. [PubMed:9228014]

Details5. Solute carrier family 22 member 8

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name: SLC22A8
Uniprot ID: Q8TCC7
Uniprot Name: Solute carrier family 22 member 8
Molecular Weight: 59855.585 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]
Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. [PubMed:14762099]
Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. [PubMed:15100168]

Details6. Solute carrier family 22 member 11

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name: SLC22A11
Uniprot ID: Q9NSA0
Uniprot Name: Solute carrier family 22 member 11
Molecular Weight: 59970.945 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]

Details7. Solute carrier family 22 member 7

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
Gene Name: SLC22A7
Uniprot ID: Q9Y694
Uniprot Name: Solute carrier family 22 member 7
Molecular Weight: 60025.025 Da

References

Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H: Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8. [PubMed:11907186]
Kobayashi Y, Ohshiro N, Shibusawa A, Sasaki T, Tokuyama S, Sekine T, Endou H, Yamamoto T: Isolation, characterization and differential gene expression of multispecific organic anion transporter 2 in mice. Mol Pharmacol. 2002 Jul;62(1):7-14. [PubMed:12065749]
Sekine T, Cha SH, Tsuda M, Apiwattanakul N, Nakajima N, Kanai Y, Endou H: Identification of multispecific organic anion transporter 2 expressed predominantly in the liver. FEBS Lett. 1998 Jun 12;429(2):179-82. [PubMed:9650585]
Morita N, Kusuhara H, Sekine T, Endou H, Sugiyama Y: Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1179-84. [PubMed:11504818]

Details8. Multidrug resistance-associated protein 4

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Atpase activity, coupled to transmembrane movement of substances
Specific Function: May be an organic anion pump relevant to cellular detoxification.
Gene Name: ABCC4
Uniprot ID: O15439
Uniprot Name: Multidrug resistance-associated protein 4
Molecular Weight: 149525.33 Da

References

Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. [PubMed:12835412]

Details9. Solute carrier organic anion transporter family member 2B1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name: SLCO2B1
Uniprot ID: O94956
Uniprot Name: Solute carrier organic anion transporter family member 2B1
Molecular Weight: 76709.98 Da

References

Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]
Nishio T, Adachi H, Nakagomi R, Tokui T, Sato E, Tanemoto M, Fujiwara K, Okabe M, Onogawa T, Suzuki T, Nakai D, Shiiba K, Suzuki M, Ohtani H, Kondo Y, Unno M, Ito S, Iinuma K, Nunoki K, Matsuno S, Abe T: Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate. Biochem Biophys Res Commun. 2000 Sep 7;275(3):831-8. [PubMed:10973807]

Details10. Solute carrier organic anion transporter family member 1A2

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name: SLCO1A2
Uniprot ID: P46721
Uniprot Name: Solute carrier organic anion transporter family member 1A2
Molecular Weight: 74144.105 Da

References

Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Cattori V, van Montfoort JE, Stieger B, Landmann L, Meijer DK, Winterhalter KH, Meier PJ, Hagenbuch B: Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95. [PubMed:11713643]
Kanai N, Lu R, Bao Y, Wolkoff AW, Schuster VL: Transient expression of oatp organic anion transporter in mammalian cells: identification of candidate substrates. Am J Physiol. 1996 Feb;270(2 Pt 2):F319-25. [PubMed:8779893]

Details11. Organic solute transporter subunit alpha

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Transporter activity
Specific Function: Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
Gene Name: SLC51A
Uniprot ID: Q86UW1
Uniprot Name: Organic solute transporter subunit alpha
Molecular Weight: 37734.575 Da

References

Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432]

Details12. Organic solute transporter subunit beta

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Transporter activity
Specific Function: Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
Gene Name: SLC51B
Uniprot ID: Q86UW2
Uniprot Name: Organic solute transporter subunit beta
Molecular Weight: 14346.195 Da

References

Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	>10000	N/A	N/A	10634944

Details13. Solute carrier organic anion transporter family member 2A1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: May mediate the release of newly synthesized prostaglandins from cells, the transepithelial transport of prostaglandins, and the clearance of prostaglandins from the circulation. Transports PGD2, a...
Gene Name: SLCO2A1
Uniprot ID: Q92959
Uniprot Name: Solute carrier organic anion transporter family member 2A1
Molecular Weight: 70043.33 Da

References

Lu R, Kanai N, Bao Y, Schuster VL: Cloning, in vitro expression, and tissue distribution of a human prostaglandin transporter cDNA(hPGT). J Clin Invest. 1996 Sep 1;98(5):1142-9. [PubMed:8787677]
Kanai N, Lu R, Satriano JA, Bao Y, Wolkoff AW, Schuster VL: Identification and characterization of a prostaglandin transporter. Science. 1995 May 12;268(5212):866-9. [PubMed:7754369]

Details14. Solute carrier organic anion transporter family member 4A1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Thyroid hormone transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name: SLCO4A1
Uniprot ID: Q96BD0
Uniprot Name: Solute carrier organic anion transporter family member 4A1
Molecular Weight: 77192.505 Da

References

Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]

Details15. Solute carrier organic anion transporter family member 1C1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Thyroid hormone transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-gluc...
Gene Name: SLCO1C1
Uniprot ID: Q9NYB5
Uniprot Name: Solute carrier organic anion transporter family member 1C1
Molecular Weight: 78695.625 Da

References

Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693]

Details16. Solute carrier organic anion transporter family member 3A1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as estrone-3-sulfate (PubMed:10873595). Mediates transport of prostaglandins (PG) E1 and E2, thyroxine (T4), deltorphin II, BQ-123 an...
Gene Name: SLCO3A1
Uniprot ID: Q9UIG8
Uniprot Name: Solute carrier organic anion transporter family member 3A1
Molecular Weight: 76552.135 Da

References

Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]
Adachi H, Suzuki T, Abe M, Asano N, Mizutamari H, Tanemoto M, Nishio T, Onogawa T, Toyohara T, Kasai S, Satoh F, Suzuki M, Tokui T, Unno M, Shimosegawa T, Matsuno S, Ito S, Abe T: Molecular characterization of human and rat organic anion transporter OATP-D. Am J Physiol Renal Physiol. 2003 Dec;285(6):F1188-97. [PubMed:14631946]

Details17. Solute carrier organic anion transporter family member 1B1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name: SLCO1B1
Uniprot ID: Q9Y6L6
Uniprot Name: Solute carrier organic anion transporter family member 1B1
Molecular Weight: 76447.99 Da

References

Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]
Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, Nomura H, Unno M, Suzuki M, Naitoh T, Matsuno S, Yawo H: Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem. 1999 Jun 11;274(24):17159-63. [PubMed:10358072]
Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]

Drug created on June 13, 2005 07:24 / Updated on September 22, 2018 22:28

Dinoprostone

Identification

Structure for Dinoprostone (DB00917)

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Clinical Trials

Pharmacoeconomics

Properties

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Enzymes

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Transporters

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