Identification
- Summary
Pranlukast is a leukotriene receptor antagonist for the treatment of allergic rhinitis and asthma symptoms.
- Generic Name
- Pranlukast
- DrugBank Accession Number
- DB01411
- Background
Pranlukast is a cysteinyl leukotriene receptor-1 antagonist. It antagonizes or reduces bronchospasm caused, principally in asthmatics, by an allergic reaction to accidentally or inadvertently encountered allergens.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Pranlukast (DB01411)
- Weight
- Average: 481.512
Monoisotopic: 481.175004241 - Chemical Formula
- C27H23N5O4
- Synonyms
- Pranlukast
- External IDs
- CCN 00401
- CCN-00401
- ONO 1078
- ONO-1078
- ONO-RS 411
- RS 411
- RS-411
- SB 205312
- SB-205312
Pharmacology
- Indication
Used as an adjunct to the standard therapy of inhaled steroids with inhaled long- and/or short-acting beta-agonists.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Allergic rhinitis (ar) •••••••••••• ••••••• ••• ••••••••• •••••• Treatment of Allergic rhinitis (ar) •••••••••••• Treatment of Asthma •••••••••••• ••••••• ••• ••••••••• •••••• - 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
Pranlukast is a cysteinyl leukotriene receptor-1 antagonist.
- Mechanism of action
Pranlukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Pranlukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.
Target Actions Organism ACysteinyl leukotriene receptor 1 antagonistHumans UTumor necrosis factor other/unknownHumans UInterleukin-5 antagonistHumans UEosinophil cationic protein other/unknownHumans UNuclear factor NF-kappa-B p105 subunit other/unknownHumans UMucin-2 other/unknownHumans UNuclear factor NF-kappa-B inhibitorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Hepatic
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- 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
Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.
- 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 softwareAbametapir The serum concentration of Pranlukast can be increased when it is combined with Abametapir. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Pranlukast. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Pranlukast. Acetohexamide The metabolism of Acetohexamide can be decreased when combined with Pranlukast. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be decreased when combined with Pranlukast. - Food Interactions
- Not Available
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 Pranlukast hydrate FR702N558K 150821-03-7 MSXTUBJFNBZPGC-UHFFFAOYSA-N
Categories
- ATC Codes
- R03DC02 — Pranlukast
- Drug Categories
- Agents to Treat Airway Disease
- Anti-Asthmatic Agents
- Benzopyrans
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs for Obstructive Airway Diseases
- Heterocyclic Compounds, Fused-Ring
- Hormone Antagonists
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Leukotriene Antagonists
- Pyrans
- Respiratory System Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as chromones. These are compounds containing a benzopyran-4-one moiety.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzopyrans
- Sub Class
- 1-benzopyrans
- Direct Parent
- Chromones
- Alternative Parents
- Benzamides / Phenoxy compounds / Phenol ethers / Benzoyl derivatives / Pyranones and derivatives / Alkyl aryl ethers / Tetrazoles / Heteroaromatic compounds / Secondary carboxylic acid amides / Oxacyclic compounds show 5 more
- Substituents
- Alkyl aryl ether / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzamide / Benzenoid / Benzoic acid or derivatives / Benzoyl / Carboxamide group / Carboxylic acid derivative show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- TB8Z891092
- CAS number
- 103177-37-3
- InChI Key
- NBQKINXMPLXUET-UHFFFAOYSA-N
- InChI
- InChI=1S/C27H23N5O4/c33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18/h1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32)
- IUPAC Name
- N-[4-oxo-2-(2H-1,2,3,4-tetrazol-5-yl)-4H-chromen-8-yl]-4-(4-phenylbutoxy)benzamide
- SMILES
- O=C(NC1=C2OC(=CC(=O)C2=CC=C1)C1=NNN=N1)C1=CC=C(OCCCCC2=CC=CC=C2)C=C1
References
- Synthesis Reference
Seiei Sasatani, Masashi Shiota, Yoshinori Ii, "Granules containing pranlukast, process for producing the granules, and method of improving adhesiveness of pranlukast." U.S. Patent US5876760, issued March, 1995.
US5876760- General References
- External Links
- PubChem Compound
- 4887
- PubChem Substance
- 46508129
- ChemSpider
- 4718
- BindingDB
- 50023198
- ChEBI
- 94810
- ChEMBL
- CHEMBL21333
- ZINC
- ZINC000001542146
- Therapeutic Targets Database
- DAP000977
- PharmGKB
- PA134698661
- PDBe Ligand
- KNT
- Wikipedia
- Pranlukast
- PDB Entries
- 6rz4
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 3 Completed Treatment Chronic Sinusitis 1 3 Completed Treatment Seasonal Allergic Rhinitis 1 1 Unknown Status Treatment Healthy Subjects (HS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder Oral Capsule Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0032 mg/mL ALOGPS logP 4.82 ALOGPS logP 4.67 Chemaxon logS -5.2 ALOGPS pKa (Strongest Acidic) 6.86 Chemaxon pKa (Strongest Basic) -1.7 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 119.09 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 139.15 m3·mol-1 Chemaxon Polarizability 51.41 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.991 Blood Brain Barrier + 0.9446 Caco-2 permeable - 0.6689 P-glycoprotein substrate Non-substrate 0.5976 P-glycoprotein inhibitor I Non-inhibitor 0.719 P-glycoprotein inhibitor II Non-inhibitor 0.6885 Renal organic cation transporter Non-inhibitor 0.8511 CYP450 2C9 substrate Non-substrate 0.8643 CYP450 2D6 substrate Non-substrate 0.8403 CYP450 3A4 substrate Non-substrate 0.5077 CYP450 1A2 substrate Non-inhibitor 0.7009 CYP450 2C9 inhibitor Non-inhibitor 0.5597 CYP450 2D6 inhibitor Non-inhibitor 0.8714 CYP450 2C19 inhibitor Non-inhibitor 0.5194 CYP450 3A4 inhibitor Non-inhibitor 0.5679 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6646 Ames test AMES toxic 0.5986 Carcinogenicity Non-carcinogens 0.875 Biodegradation Not ready biodegradable 0.997 Rat acute toxicity 2.2158 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7439 hERG inhibition (predictor II) Non-inhibitor 0.7501
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-1340900000-56f64f3c9e341a9e0dee Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001r-0005900000-b18c3becb89797a689c9 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-1511900000-3ba61725c3b435b5629d Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00l7-9314500000-03d16a78e7ba240a76ce Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-000x-9610700000-5606846bc3cbed27bfc6 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0019-4435900000-51aed43770663045dd4e 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]- 235.9053621 predictedDarkChem Lite v0.1.0 [M-H]- 200.57753 predictedDeepCCS 1.0 (2019) [M+H]+ 238.9091621 predictedDarkChem Lite v0.1.0 [M+H]+ 202.9731 predictedDeepCCS 1.0 (2019) [M+Na]+ 237.3226621 predictedDarkChem Lite v0.1.0 [M+Na]+ 208.88562 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Leukotriene receptor activity
- Specific Function
- Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, e...
- Gene Name
- CYSLTR1
- Uniprot ID
- Q9Y271
- Uniprot Name
- Cysteinyl leukotriene receptor 1
- Molecular Weight
- 38540.55 Da
References
- Yoo SH, Park SH, Song JS, Kang KH, Park CS, Yoo JH, Choi BW, Hahn MH: Clinical effects of pranlukast, an oral leukotriene receptor antagonist, in mild-to-moderate asthma: a 4 week randomized multicentre controlled trial. Respirology. 2001 Mar;6(1):15-21. [Article]
- Ogasawara H, Ishii S, Yokomizo T, Kakinuma T, Komine M, Tamaki K, Shimizu T, Izumi T: Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2: differential pharmacological properties and tissue distribution. J Biol Chem. 2002 May 24;277(21):18763-8. Epub 2002 Feb 19. [Article]
- Ishinaga H, Takeuchi K, Kishioka C, Suzuki S, Basbaum C, Majima Y: Pranlukast inhibits NF-kappaB activation and MUC2 gene expression in cultured human epithelial cells. Pharmacology. 2005 Feb;73(2):89-96. Epub 2004 Oct 5. [Article]
- Shirasaki H, Kanaizumi E, Seki N, Kikuchi M, Watanabe K, Konno N, Himi T: Distribution of specific binding sites for cysteinyl leukotriene 1 receptor antagonist in human nasal mucosa. Acta Otolaryngol. 2006 Sep;126(9):948-51. [Article]
- Ding Q, Wei EQ, Zhang YJ, Zhang WP, Chen Z: Cysteinyl leukotriene receptor 1 is involved in N-methyl-D-aspartate-mediated neuronal injury in mice. Acta Pharmacol Sin. 2006 Dec;27(12):1526-36. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Singh RK, Tandon R, Dastidar SG, Ray A: A review on leukotrienes and their receptors with reference to asthma. J Asthma. 2013 Nov;50(9):922-31. doi: 10.3109/02770903.2013.823447. Epub 2013 Aug 16. [Article]
- Suzuki S, Takeuchi K, Ishinaga H, Basbaum C, Majima Y: Leukotriene D4 upregulates MUC2 gene transcription in human epithelial cells. Pharmacology. 2008;81(3):221-8. doi: 10.1159/000112866. Epub 2008 Jan 7. [Article]
- Haneda Y, Hasegawa S, Hirano R, Hashimoto K, Ohsaki A, Ichiyama T: Leukotriene D4 enhances tumor necrosis factor-alpha-induced vascular endothelial growth factor production in human monocytes/macrophages. Cytokine. 2011 Jul;55(1):24-8. doi: 10.1016/j.cyto.2011.03.018. Epub 2011 Apr 8. [Article]
- Ichiyama T, Hasegawa S, Umeda M, Terai K, Matsubara T, Furukawa S: Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Clin Exp Allergy. 2003 Jun;33(6):802-7. [Article]
- Saito K, Nagata M, Kikuchi I, Sakamoto Y: Leukotriene D4 and eosinophil transendothelial migration, superoxide generation, and degranulation via beta2 integrin. Ann Allergy Asthma Immunol. 2004 Dec;93(6):594-600. doi: 10.1016/S1081-1206(10)61269-0. [Article]
- Figueroa EE, Kramer M, Strange K, Denton JS: CysLT1 receptor antagonists pranlukast and zafirlukast inhibit LRRC8-mediated volume regulated anion channels independently of the receptor. Am J Physiol Cell Physiol. 2019 Oct 1;317(4):C857-C866. doi: 10.1152/ajpcell.00281.2019. Epub 2019 Aug 7. [Article]
- Reques FG, Rodriguez JL: Tolerability of leukotriene modifiers in asthma: a review of clinical experience. BioDrugs. 1999 Jun;11(6):385-94. doi: 10.2165/00063030-199911060-00003. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Tumor necrosis factor receptor binding
- Specific Function
- Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct ac...
- Gene Name
- TNF
- Uniprot ID
- P01375
- Uniprot Name
- Tumor necrosis factor
- Molecular Weight
- 25644.15 Da
References
- Tomari S, Matsuse H, Machida I, Kondo Y, Kawano T, Obase Y, Fukushima C, Shimoda T, Kohno S: Pranlukast, a cysteinyl leukotriene receptor 1 antagonist, attenuates allergen-specific tumour necrosis factor alpha production and nuclear factor kappa B nuclear translocation in peripheral blood monocytes from atopic asthmatics. Clin Exp Allergy. 2003 Jun;33(6):795-801. [Article]
- Ichiyama T, Hasegawa S, Umeda M, Terai K, Matsubara T, Furukawa S: Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Clin Exp Allergy. 2003 Jun;33(6):802-7. [Article]
- Ichiyama T, Kajimoto M, Hasegawa M, Hashimoto K, Matsubara T, Furukawa S: Cysteinyl leukotrienes enhance tumour necrosis factor-alpha-induced matrix metalloproteinase-9 in human monocytes/macrophages. Clin Exp Allergy. 2007 Apr;37(4):608-14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Interleukin-5 receptor binding
- Specific Function
- Factor that induces terminal differentiation of late-developing B-cells to immunoglobulin secreting cells.
- Gene Name
- IL5
- Uniprot ID
- P05113
- Uniprot Name
- Interleukin-5
- Molecular Weight
- 15237.695 Da
References
- Hojo M, Suzuki M, Maghni K, Hamid Q, Powell WS, Martin JG: Role of cysteinyl leukotrienes in CD4(+) T cell-driven late allergic airway responses. J Pharmacol Exp Ther. 2000 May;293(2):410-6. [Article]
- Nabe T, Yamashita K, Miura M, Kawai T, Kohno S: Cysteinyl leukotriene-dependent interleukin-5 production leading to eosinophilia during late asthmatic response in guinea-pigs. Clin Exp Allergy. 2002 Apr;32(4):633-40. [Article]
- Nogimura M, Nagata M, Sutani A, Saito K, Sakamoto Y: [Study on the effect of cysteinyl leukotriene antagonist, pranlukast hydrate, on adhesive interaction between eosinophils and pulmonary endothelial cells]. Nihon Kokyuki Gakkai Zasshi. 2002 Dec;40(12):919-24. [Article]
- Fukushima C, Matsuse H, Hishikawa Y, Kondo Y, Machida I, Saeki S, Kawano T, Tomari S, Obase Y, Shimoda T, Koji T, Kohno S: Pranlukast, a leukotriene receptor antagonist, inhibits interleukin-5 production via a mechanism distinct from leukotriene receptor antagonism. Int Arch Allergy Immunol. 2005 Feb;136(2):165-72. Epub 2005 Jan 12. [Article]
- Matsuse H, Kondo Y, Machida I, Kawano T, Saeki S, Tomari S, Obase Y, Fukushima C, Mizuta Y, Kohno S: Effects of anti-inflammatory therapies on recurrent and low-grade respiratory syncytial virus infections in a murine model of asthma. Ann Allergy Asthma Immunol. 2006 Jul;97(1):55-60. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Ribonuclease activity
- Specific Function
- Cytotoxin and helminthotoxin with low-efficiency ribonuclease activity. Possesses a wide variety of biological activities. Exhibits antibacterial activity, including cytoplasmic membrane depolariza...
- Gene Name
- RNASE3
- Uniprot ID
- P12724
- Uniprot Name
- Eosinophil cationic protein
- Molecular Weight
- 18385.145 Da
References
- Horiguchi T, Tachikawa S, Kasahara J, Doi M, Shiga M: Effects of pranlukast hydrate on serum eosinophil cationic protein levels in patients with adult bronchial asthma. Arzneimittelforschung. 1999 Jan;49(1):35-7. [Article]
- Ishioka S, Hozawa S, Haruta Y, Hiyama K, Maeda A, Yamakido M: Pranlukast, a cysteinyl leukotriene antagonist, reduces serum eosinophil cationic protein levels in patients with asthma. Hiroshima J Med Sci. 1999 Dec;48(4):105-10. [Article]
- Obase Y, Shimoda T, Tomari S, Mitsuta K, Fukushima C, Kawano T, Matsuse H, Kohno S: Effects of pranlukast on aspirin-induced bronchoconstriction: differences in chemical mediators between aspirin-intolerant and tolerant asthmatic patients. Ann Allergy Asthma Immunol. 2001 Jul;87(1):74-9. [Article]
- Kanazawa H, Yoshikawa T, Hirata K, Yoshikawa J: Effects of pranlukast administration on vascular endothelial growth factor levels in asthmatic patients. Chest. 2004 May;125(5):1700-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Transcriptional repressor activity, rna polymerase ii transcription regulatory region sequence-specific binding
- Specific Function
- NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
- Gene Name
- NFKB1
- Uniprot ID
- P19838
- Uniprot Name
- Nuclear factor NF-kappa-B p105 subunit
- Molecular Weight
- 105355.175 Da
References
- Tomari S, Matsuse H, Machida I, Kondo Y, Kawano T, Obase Y, Fukushima C, Shimoda T, Kohno S: Pranlukast, a cysteinyl leukotriene receptor 1 antagonist, attenuates allergen-specific tumour necrosis factor alpha production and nuclear factor kappa B nuclear translocation in peripheral blood monocytes from atopic asthmatics. Clin Exp Allergy. 2003 Jun;33(6):795-801. [Article]
- Ichiyama T, Hasegawa S, Umeda M, Terai K, Matsubara T, Furukawa S: Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Clin Exp Allergy. 2003 Jun;33(6):802-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Not Available
- Specific Function
- Coats the epithelia of the intestines, airways, and other mucus membrane-containing organs. Thought to provide a protective, lubricating barrier against particles and infectious agents at mucosal s...
- Gene Name
- MUC2
- Uniprot ID
- Q02817
- Uniprot Name
- Mucin-2
- Molecular Weight
- 540296.38 Da
References
- Ishinaga H, Takeuchi K, Kishioka C, Suzuki S, Basbaum C, Majima Y: Pranlukast inhibits NF-kappaB activation and MUC2 gene expression in cultured human epithelial cells. Pharmacology. 2005 Feb;73(2):89-96. Epub 2004 Oct 5. [Article]
- Bai CH, Song SY, Kim YD: The inhibitory effect of the leukotriene receptor antagonist on leukotriene D4-induced MUC2/5AC gene expression and mucin secretion in human airway epithelial cells. Auris Nasus Larynx. 2007 Jun;34(2):203-6. Epub 2007 Jan 12. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
- Specific Function
- NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
Components:
| Name | UniProt ID |
|---|---|
| Nuclear factor NF-kappa-B p100 subunit | Q00653 |
| Nuclear factor NF-kappa-B p105 subunit | P19838 |
References
- Ichiyama T, Hasegawa S, Umeda M, Terai K, Matsubara T, Furukawa S: Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Clin Exp Allergy. 2003 Jun;33(6):802-7. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Data supporting this enzyme action are limited to the findings of 1 in vitro study.
- General Function
- Steroid hydroxylase activity
- 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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Liu KH, Lee YM, Shon JH, Kim MJ, Lee SS, Yoon YR, Cha IJ, Shin JG: Potential of pranlukast and zafirlukast in the inhibition of human liver cytochrome P450 enzymes. Xenobiotica. 2004 May;34(5):429-38. doi: 10.1080/00498250410001691253 . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- 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 performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Nakade S, Yamauchi A, Komaba J, Ohno T, Kitagawa J, Honda N, Hasegawa C, Yoneda K, Kodama Y, Yasuda K, Azuma J, Miyata Y: Effect of clarithromycin on the pharmacokinetics of pranlukast in healthy volunteers. Drug Metab Pharmacokinet. 2008;23(6):428-33. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Horikawa M, Kato Y, Tyson CA, Sugiyama Y: The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites. Drug Metab Pharmacokinet. 2002;17(1):23-33. [Article]
Drug created at July 17, 2007 12:39 / Updated at June 12, 2021 10:52