Identification
- Summary
Iloprost is a synthetic prostacyclin analog indicated to treat pulmonary arterial hypertension (PAH).
- Brand Names
- Ventavis
- Generic Name
- Iloprost
- DrugBank Accession Number
- DB01088
- Background
Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It is used to treat pulmonary arterial hypertension (PAH).
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Iloprost (DB01088)
- Weight
- Average: 360.494
Monoisotopic: 360.23005951 - Chemical Formula
- C22H32O4
- Synonyms
- Iloprost
Pharmacology
- Indication
Used for the treatment of pulmonary arterial hypertension.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Nyha class iii pulmonary arterial hypertension •••••••••••• Management of Nyha class iv pulmonary arterial hypertension •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It was shown to affect platelet aggregation, but whether this effect contributes to its vasodilatory action has not been elucidated. There are two diastereoisomers of iloprost and the 4S isomer is reported to exhibit a higher potency in dilating blood vessels compared to the 4R isomer.
- Mechanism of action
Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, such as carbaprostacyclin. Iloprost binds with equal affinity to human prostacyclin (Prostanoid IP) and prostaglandin EP1 receptors. Iloprost constricts the ilium and fundus circular smooth muscle as strongly as prostaglandin E2 (PGE2) itself. Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time. All of these properties help to antagonize the pathological changes that take place in the small pulmonary arteries of patients with pulmonary hypertension.
Target Actions Organism AProstacyclin receptor agonistHumans AProstaglandin E2 receptor EP1 subtype agonistHumans UcAMP-specific 3',5'-cyclic phosphodiesterase 4A inducerHumans UcAMP-specific 3',5'-cyclic phosphodiesterase 4B inducerHumans UcAMP-specific 3',5'-cyclic phosphodiesterase 4C inducerHumans UcAMP-specific 3',5'-cyclic phosphodiesterase 4D inducerHumans UTissue-type plasminogen activator other/unknownHumans UProstaglandin D2 receptor 2 agonistHumans - Absorption
Rapidly absorbed with bioavailability of 63%
- Volume of distribution
- 0.7 to 0.8 L/kg
- Protein binding
60%
- Metabolism
Primarily hepatic. Iloprost is metabolized principally via beta-oxidation of the carboxyl side chain.
- Route of elimination
Not Available
- Half-life
20-30 minutes
- Clearance
- 20 mL/min/kg [Normal subjects]
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Overdoses can lead to hypotension, headache, flushing, nausea, vomiting, and diarrhea.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide The risk or severity of adverse effects can be increased when Iloprost is combined with Abaloparatide. Abciximab The risk or severity of bleeding can be increased when Iloprost is combined with Abciximab. Abrocitinib The risk or severity of bleeding and thrombocytopenia can be increased when Iloprost is combined with Abrocitinib. Acebutolol Iloprost may increase the hypotensive activities of Acebutolol. Aceclofenac The risk or severity of bleeding can be increased when Aceclofenac is combined with Iloprost. - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Taking iloprost with anticoagulant/antiplatelet herbs may increase the risk of bleeding occurring as an adverse effect. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Iloprost tromethamine 807T91913V 697225-02-8 KZSSWXACMCYLBM-RMWNCEGRSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ventavis Solution 20 μg/ml Respiratory (inhalation) Bayer Ag 2016-09-08 Not applicable EU 
Ventavis Solution 10 μg/ml Respiratory (inhalation) Bayer Ag 2016-09-08 Not applicable EU Ventavis Solution 10 μg/ml Respiratory (inhalation) Bayer Ag 2016-09-08 Not applicable EU Ventavis Solution 10 μg/ml Respiratory (inhalation) Bayer Ag 2016-09-08 Not applicable EU Ventavis Solution 20 μg/ml Respiratory (inhalation) Bayer Ag 2016-09-08 Not applicable EU
Categories
- ATC Codes
- B01AC11 — Iloprost
- Drug Categories
- Agents Causing Muscle Toxicity
- Antiplatelet agents
- Autacoids
- Biological Factors
- Blood and Blood Forming Organs
- Cardiovascular Agents
- Eicosanoids
- Fatty Acids
- Fatty Acids, Unsaturated
- Hematologic Agents
- Hypotensive Agents
- Inflammation Mediators
- Lipids
- OATP2B1/SLCO2B1 substrates
- Platelet Aggregation Inhibitors Excl. Heparin
- Prostacyclin Analogues
- Prostaglandins
- Prostaglandins, Synthetic
- Vasodilating Agents
- 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
- Bicyclic monoterpenoids / Medium-chain hydroxy acids and derivatives / Fatty alcohols / Medium-chain fatty acids / Hydroxy fatty acids / Branched fatty acids / Secondary alcohols / Cyclic alcohols and derivatives / Monocarboxylic acids and derivatives / Carboxylic acids show 3 more
- Substituents
- Alcohol / Aliphatic homopolycyclic compound / Bicyclic monoterpenoid / Branched fatty acid / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Cyclic alcohol / Fatty alcohol / Hydrocarbon derivative show 10 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- monocarboxylic acid, secondary alcohol, carbobicyclic compound (CHEBI:63916)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- JED5K35YGL
- CAS number
- 78919-13-8
- InChI Key
- HIFJCPQKFCZDDL-ACWOEMLNSA-N
- InChI
- InChI=1S/C22H32O4/c1-3-4-7-15(2)20(23)11-10-18-19-13-16(8-5-6-9-22(25)26)12-17(19)14-21(18)24/h8,10-11,15,17-21,23-24H,5-7,9,12-14H2,1-2H3,(H,25,26)/b11-10+,16-8+/t15?,17-,18+,19-,20+,21+/m0/s1
- IUPAC Name
- 5-[(2E,3aS,4R,5R,6aS)-5-hydroxy-4-[(1E,3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl]-octahydropentalen-2-ylidene]pentanoic acid
- SMILES
- [H][C@]12C[C@@H](O)[C@H](\C=C\[C@@H](O)C(C)CC#CC)[C@@]1([H])C\C(C2)=C\CCCC(O)=O
References
- General References
- Not Available
- External Links
- PubChem Compound
- 5311181
- PubChem Substance
- 46507818
- ChemSpider
- 4470703
- BindingDB
- 23954
- 40138
- ChEBI
- 63916
- ChEMBL
- CHEMBL494
- Therapeutic Targets Database
- DAP000273
- PharmGKB
- PA164746843
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Iloprost
- FDA label
- Download (244 KB)
- MSDS
- Download (67.1 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Peripheral Arterial Disease (PAD) 1 4 Completed Treatment Pulmonary Arterial Hypertension (PAH) / Sarcoidosis 1 4 Terminated Diagnostic Pulmonary Hypertension (PH) 1 4 Terminated Treatment Hypertension 1 4 Terminated Treatment Pulmonary Hypertension (PH) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Actelion Pharmaceuticals Inc.
- Berlimed Sa
- Cotherix Inc.
- Dosage Forms
Form Route Strength Injection, solution, concentrate Cutaneous; Intravenous 0.05 MG/0.5ML Injection, solution, concentrate Intravenous Injection, solution, concentrate Intravenous 0.05 MG/0.5ML Injection, solution, concentrate Intravenous 0100 MG/1ML Injection Intravenous Concentrate Intravenous Injection, solution Intravenous 20 mcg/ml Injection, solution, concentrate Intravenous 50 mcg/0.5ml Solution Respiratory (inhalation) Solution Respiratory (inhalation) 20 MICROGRAMMI/ML Solution Respiratory (inhalation) 10 Mikrogramm/ml Injection, solution, concentrate Intravenous 20 Mikrogramm/ml Solution Respiratory (inhalation) 20 Mikrogramm/ml Injection, solution, concentrate Intravenous 100 MICROGRAMMI/ML Injection, solution Intravenous 20 mcg/2ml Injection, solution Intravenous Aerosol Respiratory (inhalation) Solution Respiratory (inhalation) 0.01 mg/1mL Solution Respiratory (inhalation) 0.013 mg Solution Respiratory (inhalation) 0.02 mg/1mL Solution Respiratory (inhalation) 10 ug/1mL Solution Respiratory (inhalation) 10 μg/ml Solution Respiratory (inhalation) 10 ?g/ml Solution Respiratory (inhalation) 20 MCG/ML Solution Respiratory (inhalation) 20 ?g/ml Solution Respiratory (inhalation) 20 μg/ml Solution Respiratory (inhalation) 20 mcg Solution Respiratory (inhalation) 2000000 mcg Solution Respiratory (inhalation) 10 mcg/ml Solution Nasal 0.010 mg/ml Solution Respiratory (inhalation) 20 cg Aerosol Respiratory (inhalation) 0.01 mg/1ml - Prices
Unit description Cost Unit Ventavis 10 mcg/1 ml solution 74.4USD ml Ventavis 20 mcg/1 ml solution 74.4USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Very slightly soluble Not Available logP 4.8 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00874 mg/mL ALOGPS logP 4.22 ALOGPS logP 3.56 Chemaxon logS -4.6 ALOGPS pKa (Strongest Acidic) 4.66 Chemaxon pKa (Strongest Basic) -0.87 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 77.76 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 105.18 m3·mol-1 Chemaxon Polarizability 42.68 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9543 Blood Brain Barrier + 0.5506 Caco-2 permeable + 0.5 P-glycoprotein substrate Substrate 0.7459 P-glycoprotein inhibitor I Non-inhibitor 0.6507 P-glycoprotein inhibitor II Non-inhibitor 0.8227 Renal organic cation transporter Non-inhibitor 0.8698 CYP450 2C9 substrate Non-substrate 0.8526 CYP450 2D6 substrate Non-substrate 0.8946 CYP450 3A4 substrate Substrate 0.6553 CYP450 1A2 substrate Non-inhibitor 0.5515 CYP450 2C9 inhibitor Non-inhibitor 0.7963 CYP450 2D6 inhibitor Non-inhibitor 0.8072 CYP450 2C19 inhibitor Non-inhibitor 0.719 CYP450 3A4 inhibitor Inhibitor 0.5377 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7556 Ames test Non AMES toxic 0.7104 Carcinogenicity Non-carcinogens 0.9587 Biodegradation Not ready biodegradable 0.6052 Rat acute toxicity 2.7260 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9288 hERG inhibition (predictor II) Non-inhibitor 0.6964
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-004i-0029000000-31b136be94039d233232 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0009000000-3d97279dd73ca80d8993 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-052f-1169000000-95bcd53b77c6621a63f0 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-004i-1298000000-c14f4b9c28e606770fca Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0bt9-2169000000-c1dfe93cc6985f9524ff Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0fri-9740000000-e45bbe51efc93c8930c7 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 194.31767 predictedDeepCCS 1.0 (2019) [M+H]+ 196.87813 predictedDeepCCS 1.0 (2019) [M+Na]+ 204.19557 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- Receptor for prostacyclin (prostaglandin I2 or PGI2). The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase.
- Gene Name
- PTGIR
- Uniprot ID
- P43119
- Uniprot Name
- Prostacyclin receptor
- Molecular Weight
- 40955.485 Da
References
- Takamatsu H, Tsukada H, Watanabe Y, Cui Y, Kataoka Y, Hosoya T, Suzuki M, Watanabe Y: Specific ligand for a central type prostacyclin receptor attenuates neuronal damage in a rat model of focal cerebral ischemia. Brain Res. 2002 Jan 25;925(2):176-82. [Article]
- Crutchley DJ, Solomon DE, Conanan LB: Prostacyclin analogues inhibit tissue factor expression in the human monocytic cell line THP-1 via a cyclic AMP-dependent mechanism. Arterioscler Thromb. 1992 Jun;12(6):664-70. [Article]
- Schermuly RT, Pullamsetti SS, Breitenbach SC, Weissmann N, Ghofrani HA, Grimminger F, Nilius SM, Schror K, Kirchrath JM, Seeger W, Rose F: Iloprost-induced desensitization of the prostacyclin receptor in isolated rabbit lungs. Respir Res. 2007 Jan 26;8:4. [Article]
- Idzko M, Hammad H, van Nimwegen M, Kool M, Vos N, Hoogsteden HC, Lambrecht BN: Inhaled iloprost suppresses the cardinal features of asthma via inhibition of airway dendritic cell function. J Clin Invest. 2007 Feb;117(2):464-72. [Article]
- Tsai AL, Vijjeswarapu H, Wu KK: Interaction between platelet receptor and iloprost isomers. Biochim Biophys Acta. 1988 Jul 21;942(2):220-6. [Article]
- Olschewski H, Rose F, Schermuly R, Ghofrani HA, Enke B, Olschewski A, Seeger W: Prostacyclin and its analogues in the treatment of pulmonary hypertension. Pharmacol Ther. 2004 May;102(2):139-53. [Article]
- Anderson JR, Nawarskas JJ: Pharmacotherapeutic management of pulmonary arterial hypertension. Cardiol Rev. 2010 May-Jun;18(3):148-62. doi: 10.1097/CRD.0b013e3181d4e921. [Article]
- Mubarak KK: A review of prostaglandin analogs in the management of patients with pulmonary arterial hypertension. Respir Med. 2010 Jan;104(1):9-21. doi: 10.1016/j.rmed.2009.07.015. Epub 2009 Aug 15. [Article]
- Krug S, Sablotzki A, Hammerschmidt S, Wirtz H, Seyfarth HJ: Inhaled iloprost for the control of pulmonary hypertension. Vasc Health Risk Manag. 2009;5(1):465-74. [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
- Sharif NA, Davis TL: Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques. J Pharm Pharmacol. 2002 Apr;54(4):539-47. [Article]
- Walch L, de Montpreville V, Brink C, Norel X: Prostanoid EP(1)- and TP-receptors involved in the contraction of human pulmonary veins. Br J Pharmacol. 2001 Dec;134(8):1671-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Metal ion binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
- Gene Name
- PDE4A
- Uniprot ID
- P27815
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4A
- Molecular Weight
- 98142.155 Da
References
- Wilkens H, Guth A, Konig J, Forestier N, Cremers B, Hennen B, Bohm M, Sybrecht GW: Effect of inhaled iloprost plus oral sildenafil in patients with primary pulmonary hypertension. Circulation. 2001 Sep 11;104(11):1218-22. [Article]
- Ghofrani HA, Rose F, Schermuly RT, Olschewski H, Wiedemann R, Weissmann N, Schudt C, Tenor H, Seeger W, Grimminger F: Amplification of the pulmonary vasodilatory response to inhaled iloprost by subthreshold phosphodiesterase types 3 and 4 inhibition in severe pulmonary hypertension. Crit Care Med. 2002 Nov;30(11):2489-92. [Article]
- Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D: Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Eur Respir J. 2003 Aug;22(2):342-7. [Article]
- Grant PG, Mannarino AF, Colman RW: cAMP-mediated phosphorylation of the low-Km cAMP phosphodiesterase markedly stimulates its catalytic activity. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9071-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Metal ion binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging f...
- Gene Name
- PDE4B
- Uniprot ID
- Q07343
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4B
- Molecular Weight
- 83342.695 Da
References
- Wilkens H, Guth A, Konig J, Forestier N, Cremers B, Hennen B, Bohm M, Sybrecht GW: Effect of inhaled iloprost plus oral sildenafil in patients with primary pulmonary hypertension. Circulation. 2001 Sep 11;104(11):1218-22. [Article]
- Ghofrani HA, Rose F, Schermuly RT, Olschewski H, Wiedemann R, Weissmann N, Schudt C, Tenor H, Seeger W, Grimminger F: Amplification of the pulmonary vasodilatory response to inhaled iloprost by subthreshold phosphodiesterase types 3 and 4 inhibition in severe pulmonary hypertension. Crit Care Med. 2002 Nov;30(11):2489-92. [Article]
- Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D: Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Eur Respir J. 2003 Aug;22(2):342-7. [Article]
- Grant PG, Mannarino AF, Colman RW: cAMP-mediated phosphorylation of the low-Km cAMP phosphodiesterase markedly stimulates its catalytic activity. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9071-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Metal ion binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
- Gene Name
- PDE4C
- Uniprot ID
- Q08493
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4C
- Molecular Weight
- 79900.795 Da
References
- Wilkens H, Guth A, Konig J, Forestier N, Cremers B, Hennen B, Bohm M, Sybrecht GW: Effect of inhaled iloprost plus oral sildenafil in patients with primary pulmonary hypertension. Circulation. 2001 Sep 11;104(11):1218-22. [Article]
- Ghofrani HA, Rose F, Schermuly RT, Olschewski H, Wiedemann R, Weissmann N, Schudt C, Tenor H, Seeger W, Grimminger F: Amplification of the pulmonary vasodilatory response to inhaled iloprost by subthreshold phosphodiesterase types 3 and 4 inhibition in severe pulmonary hypertension. Crit Care Med. 2002 Nov;30(11):2489-92. [Article]
- Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D: Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Eur Respir J. 2003 Aug;22(2):342-7. [Article]
- Grant PG, Mannarino AF, Colman RW: cAMP-mediated phosphorylation of the low-Km cAMP phosphodiesterase markedly stimulates its catalytic activity. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9071-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Ubiquitin protein ligase binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
- Gene Name
- PDE4D
- Uniprot ID
- Q08499
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4D
- Molecular Weight
- 91114.1 Da
References
- Wilkens H, Guth A, Konig J, Forestier N, Cremers B, Hennen B, Bohm M, Sybrecht GW: Effect of inhaled iloprost plus oral sildenafil in patients with primary pulmonary hypertension. Circulation. 2001 Sep 11;104(11):1218-22. [Article]
- Ghofrani HA, Rose F, Schermuly RT, Olschewski H, Wiedemann R, Weissmann N, Schudt C, Tenor H, Seeger W, Grimminger F: Amplification of the pulmonary vasodilatory response to inhaled iloprost by subthreshold phosphodiesterase types 3 and 4 inhibition in severe pulmonary hypertension. Crit Care Med. 2002 Nov;30(11):2489-92. [Article]
- Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D: Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Eur Respir J. 2003 Aug;22(2):342-7. [Article]
- Grant PG, Mannarino AF, Colman RW: cAMP-mediated phosphorylation of the low-Km cAMP phosphodiesterase markedly stimulates its catalytic activity. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9071-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Serine-type endopeptidase activity
- Specific Function
- Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single Arg-Val bond in plasminogen. By controlling plasmin-mediated proteolysis, it plays an important role in t...
- Gene Name
- PLAT
- Uniprot ID
- P00750
- Uniprot Name
- Tissue-type plasminogen activator
- Molecular Weight
- 62916.495 Da
References
- Kerins DM, Roy L, Kunitada S, Adedoyin A, FitzGerald GA, Fitzgerald DJ: Pharmacokinetics of tissue-type plasminogen activator during acute myocardial infarction in men. Effect of a prostacyclin analogue. Circulation. 1992 Feb;85(2):526-32. [Article]
- Nicolini FA, Mehta JL, Nichols WW, Saldeen TG, Grant M: Prostacyclin analogue iloprost decreases thrombolytic potential of tissue-type plasminogen activator in canine coronary thrombosis. Circulation. 1990 Mar;81(3):1115-22. [Article]
- Nichols WW, Nicolini FA, Saldeen TG, Mehta JL: Combined thrombolytic effects of tissue-plasminogen activator and a fibrinogen-degradation product peptide 6A or iloprost. J Cardiovasc Pharmacol. 1991 Aug;18(2):231-6. [Article]
- Nizankowski R, Krzanowski M, Musial J, Szczeklik A: [Effect of thromboxane A2 synthetase inhibitor and prostacyclin analogue on arterial blood pressure, fibrinolysis and platelet function in patients with hypertension]. Pol Tyg Lek. 1991 Jan 7-14;46(1-3):18-21. [Article]
- Herczenik E, Bouma B, Korporaal SJ, Strangi R, Zeng Q, Gros P, Van Eck M, Van Berkel TJ, Gebbink MF, Akkerman JW: Activation of human platelets by misfolded proteins. Arterioscler Thromb Vasc Biol. 2007 Jul;27(7):1657-65. Epub 2007 May 17. [Article]
- Kind
- Protein
- Organism
- Humans
- 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. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at May 07, 2021 21:22