Roflumilast (BioDeep_00000399055)
natural product
代谢物信息卡片
化学式: C17H14Cl2F2N2O3 (402.0349)
中文名称: 罗氟司特
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
InChI: InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24)
描述信息
R - Respiratory system > R03 - Drugs for obstructive airway diseases
C471 - Enzyme Inhibitor > C744 - Phosphodiesterase Inhibitor
同义名列表
2 个代谢物同义名
数据库引用编号
7 个数据库交叉引用编号
- ChEBI: CHEBI:47657
- KEGGdrug: D05744
- PubChem: 449193
- DrugBank: DB01656
- ChEMBL: CHEMBL193240
- CAS: 162401-32-3
- MoNA: CCMSLIB00000078452
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:
- PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称,可以跳转到相关代谢物的信息页面。
亚细胞结构定位 | 关联基因列表 |
---|
文献列表
- Riyadh S Almalki. The Protective Effect of Roflumilast Against Acute Hepatotoxicity Caused by Methotrexate in Wistar Rats: In vivo Evaluation.
Drug design, development and therapy.
2024; 18(?):453-462. doi:
10.2147/dddt.s438703
. [PMID: 38374827] - Mahmoud A Desouky, Mina Y George, Haidy E Michel, Doaa A Elsherbiny. Roflumilast escalates α-synuclein aggregate degradation in rotenone-induced Parkinson's disease in rats: Modulation of the ubiquitin-proteasome system and endoplasmic reticulum stress.
Chemico-biological interactions.
2023 Apr; 379(?):110491. doi:
10.1016/j.cbi.2023.110491
. [PMID: 37105514] - Xiaowei Ji, Yao Ye, Lin Wang, Suying Liu, Xi Dong. PDE4 inhibitor Roflumilast modulates inflammation and lipid accumulation in PCOS mice to improve ovarian function and reduce DHEA-induced granulosa cell apoptosis in vitro.
Drug development research.
2023 Jan; ?(?):. doi:
10.1002/ddr.22027
. [PMID: 36621953] - Emanuela F Craparo, Marta Cabibbo, Cinzia Scialabba, Gaetano Giammona, Gennara Cavallaro. Inhalable Formulation Based on Lipid-Polymer Hybrid Nanoparticles for the Macrophage Targeted Delivery of Roflumilast.
Biomacromolecules.
2022 08; 23(8):3439-3451. doi:
10.1021/acs.biomac.2c00576
. [PMID: 35899612] - Yogendra Singh, Neeraj Kumar Fuloria, Shivkanya Fuloria, Vetriselvan Subramaniyan, Waleed Hassan Almalki, Fahad A Al-Abbasi, Imran Kazmi, Sobhit Singh Rajput, Nirmal Joshi, Gaurav Gupta. A European pharmacotherapeutic agent roflumilast exploring integrated preclinical and clinical evidence for SARS CoV-2 mediated inflammation to organ damage.
British journal of clinical pharmacology.
2022 08; 88(8):3562-3565. doi:
10.1111/bcp.15328
. [PMID: 35352842] - Kirti Gupta, Sneha Pandey, Ragini Singh, Abha Kumari, Pallavi Sen, Gaaminepreet Singh. Roflumilast improves resolution of sepsis-induced acute kidney injury by retarding late phase renal interstitial immune cells infiltration and leakage in urinary sediments.
Fundamental & clinical pharmacology.
2022 Feb; 36(1):114-132. doi:
10.1111/fcp.12711
. [PMID: 34212425] - A Shaikh-Omar, H A Murad, N M Alotaibi. Rectal roflumilast improves trinitrobenzenesulfonic acid-induced chronic colitis in rats.
Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.
2022; 55(?):e11877. doi:
10.1590/1414-431x2021e11877
. [PMID: 35239781] - Xiang Tao, Haiqing He, Jiangtong Peng, Rui Xu, Jing Fu, Yuting Hu, Li Li, Xiaoyan Yang, Xiuling Feng, Chao Zhang, Lingmin Zhang, Xiyong Yu, Ao Shen, Kai Huang, Qin Fu. Overexpression of PDE4D in mouse liver is sufficient to trigger NAFLD and hypertension in a CD36-TGF-β1 pathway: therapeutic role of roflumilast.
Pharmacological research.
2022 01; 175(?):106004. doi:
10.1016/j.phrs.2021.106004
. [PMID: 34826603] - Shasha Zeng, Haibing Bai, Mi Zou. Effects of Roflumilast on Patients with Chronic Obstructive Pulmonary Disease Treated with Inhaled Corticosteroid/Long-Acting β2 Agonist: A Meta-analysis.
Computational and mathematical methods in medicine.
2022; 2022(?):8101099. doi:
10.1155/2022/8101099
. [PMID: 35915771] - Basel A Abdel-Wahab, Ismail A Walbi, Hassan A Albarqi, Fares E M Ali, Emad H M Hassanein. Roflumilast protects from cisplatin-induced testicular toxicity in male rats and enhances its cytotoxicity in prostate cancer cell line. Role of NF-κB-p65, cAMP/PKA and Nrf2/HO-1, NQO1 signaling.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.
2021 May; 151(?):112133. doi:
10.1016/j.fct.2021.112133
. [PMID: 33757793] - Priyanka Saroj, Yashika Bansal, Raghunath Singh, Ansab Akhtar, Rupinder Kaur Sodhi, Mahendra Bishnoi, Sangeeta Pilkhwal Sah, Anurag Kuhad. Neuroprotective effects of roflumilast against quinolinic acid-induced rat model of Huntington's disease through inhibition of NF-κB mediated neuroinflammatory markers and activation of cAMP/CREB/BDNF signaling pathway.
Inflammopharmacology.
2021 Apr; 29(2):499-511. doi:
10.1007/s10787-020-00787-3
. [PMID: 33517508] - Sugin Lal Jabaris S, Ranju V. Scope of adjuvant therapy using roflumilast, a PDE-4 inhibitor against COVID-19.
Pulmonary pharmacology & therapeutics.
2021 02; 66(?):101978. doi:
10.1016/j.pupt.2020.101978
. [PMID: 33259924] - Haijun Qu, Keyu Zhang, Chunqing Fu, Feng Qiu. Simultaneous quantification and pharmacokinetic evaluation of roflumilast and its N-oxide in cynomolgus monkey plasma by LC-MS/MS method.
Biomedical chromatography : BMC.
2021 Feb; 35(2):e4973. doi:
10.1002/bmc.4973
. [PMID: 32840886] - Wan Xu, Jingjing Zhang, Jing Xiao. Roflumilast Suppresses Adipogenic Differentiation via AMPK Mediated Pathway.
Frontiers in endocrinology.
2021; 12(?):662451. doi:
10.3389/fendo.2021.662451
. [PMID: 34163436] - Manar Mohammed El Tabaa, Maram Mohammed El Tabaa. New putative insights into neprilysin (NEP)-dependent pharmacotherapeutic role of roflumilast in treating COVID-19.
European journal of pharmacology.
2020 Dec; 889(?):173615. doi:
10.1016/j.ejphar.2020.173615
. [PMID: 33011243] - Fuying Ma, Guangping Chen, Eva L Rodriguez, Janet D Klein, Jeff M Sands, Yanhua Wang. Adrenomedullin Inhibits Osmotic Water Permeability in Rat Inner Medullary Collecting Ducts.
Cells.
2020 11; 9(12):. doi:
10.3390/cells9122533
. [PMID: 33255239] - Chirag A Shah. Can roflumilast become steroid-sparing alternative in the treatment of COVID-19?.
Medical hypotheses.
2020 Nov; 144(?):110246. doi:
10.1016/j.mehy.2020.110246
. [PMID: 33254551] - Xingkai Xu, Lulei Liao, Baisheng Hu, Hao Jiang, Meichun Tan. Roflumilast, a Phosphodiesterases-4 (PDE4) Inhibitor, Alleviates Sepsis‑induced Acute Kidney Injury.
Medical science monitor : international medical journal of experimental and clinical research.
2020 May; 26(?):e921319. doi:
10.12659/msm.921319
. [PMID: 32449901] - Rui Shi, Wei-Wei Su, Zhi-Ting Zhu, Min-Yi Guan, Ke-Ling Cheng, Wei-Yang Fan, Gu-Yi Wei, Pei-Bo Li, Zhong-Yi Yang, Hong-Liang Yao. Regulation effects of naringin on diesel particulate matter-induced abnormal airway surface liquid secretion.
Phytomedicine : international journal of phytotherapy and phytopharmacology.
2019 Oct; 63(?):153004. doi:
10.1016/j.phymed.2019.153004
. [PMID: 31301536] - Bahia A Moussa, Asmaa A El-Zaher, Mohamed K El-Ashrey, Marwa A Fouad. Roflumilast analogs with improved metabolic stability, plasma protein binding, and pharmacokinetic profile.
Drug testing and analysis.
2019 Jun; 11(6):886-897. doi:
10.1002/dta.2562
. [PMID: 30578615] - M N Ansari, R I Aloliet, M A Ganaie, T H Khan, Najeeb-Ur-Rehman, F Imam, A M Hamad. Roflumilast, a phosphodiesterase 4 inhibitor, attenuates cadmium-induced renal toxicity via modulation of NF-κB activation and induction of NQO1 in rats.
Human & experimental toxicology.
2019 May; 38(5):588-597. doi:
10.1177/0960327119829521
. [PMID: 30744402] - Honglin Ding, Peng Zhang, Ning Li, Yili Liu, Ping Wang. The phosphodiesterase type 4 inhibitor roflumilast suppresses inflammation to improve diabetic bladder dysfunction rats.
International urology and nephrology.
2019 Feb; 51(2):253-260. doi:
10.1007/s11255-018-2038-z
. [PMID: 30474782] - P Kosutova, P Mikolka, M Kolomaznik, S Balentova, M Adamkov, A Calkovska, D Mokra. Reduction of lung inflammation, oxidative stress and apoptosis by the PDE4 inhibitor roflumilast in experimental model of acute lung injury.
Physiological research.
2018 12; 67(Suppl 4):S645-S654. doi:
10.33549/physiolres.934047
. [PMID: 30607971] - Zhe Qiang, Zong-Yuan Zhou, Ting Peng, Pu-Zi Jiang, Nan Shi, Emmanuel Mfotie Njoya, Bahtigul Azimova, Wan-Li Liu, Wei-Hua Chen, Guo-Lin Zhang, Fei Wang. Inhibition of TPL2 by interferon-α suppresses bladder cancer through activation of PDE4D.
Journal of experimental & clinical cancer research : CR.
2018 Nov; 37(1):288. doi:
10.1186/s13046-018-0971-4
. [PMID: 30482227] - Martin Kertys, Anna Urbanova, Juraj Mokry. Determination of Phosphodiesterase Inhibitors Tadalafil, Roflumilast and Roflumilast N-Oxide Using LC-MS in Guinea Pig Plasma.
Journal of chromatographic science.
2018 Nov; 56(10):948-954. doi:
10.1093/chromsci/bmy072
. [PMID: 29992297] - Axel Facius, Eleonora Marostica, Philip Gardiner, Henrik Watz, Gezim Lahu. Pharmacokinetic and Pharmacodynamic Modelling to Characterize the Tolerability of Alternative Up-Titration Regimens of Roflumilast in Patients with Chronic Obstructive Pulmonary Disease.
Clinical pharmacokinetics.
2018 08; 57(8):1029-1038. doi:
10.1007/s40262-018-0671-4
. [PMID: 29797235] - Akihiro Takano, Tolga Uz, Jesus Garcia-Segovia, Max Tsai, Gezim Lahu, Nahid Amini, Ryuji Nakao, Zhisheng Jia, Christer Halldin. A Nonhuman Primate PET Study: Measurement of Brain PDE4 Occupancy by Roflumilast Using (R)-[11C]Rolipram.
Molecular imaging and biology.
2018 08; 20(4):615-622. doi:
10.1007/s11307-018-1168-0
. [PMID: 29441434] - Thomas H Sisson, Paul J Christensen, Yo Muraki, Anthony J Dils, Lauren Chibucos, Natalya Subbotina, Kimio Tohyama, Jeffrey C Horowitz, Takanori Matsuo, Marc Bailie, Sham Nikam, Masatoshi Hazama. Phosphodiesterase 4 inhibition reduces lung fibrosis following targeted type II alveolar epithelial cell injury.
Physiological reports.
2018 06; 6(12):e13753. doi:
10.14814/phy2.13753
. [PMID: 29952109] - Bahia A Moussa, Asmaa A El-Zaher, Mohamed K El-Ashrey, Marwa A Fouad. Synthesis and molecular docking of new roflumilast analogues as preferential-selective potent PDE-4B inhibitors with improved pharmacokinetic profile.
European journal of medicinal chemistry.
2018 Mar; 148(?):477-486. doi:
10.1016/j.ejmech.2018.02.038
. [PMID: 29477888] - M A Van Duinen, A Sambeth, P R A Heckman, S Smit, M Tsai, G Lahu, T Uz, A Blokland, J Prickaerts. Acute administration of roflumilast enhances immediate recall of verbal word memory in healthy young adults.
Neuropharmacology.
2018 03; 131(?):31-38. doi:
10.1016/j.neuropharm.2017.12.019
. [PMID: 29241652] - Tanveer A Wani, Ahmed H Bakheit, Mohammed Nazam Ansari, Abdul-Rahman A Al-Majed, Bakr M Al-Qahtani, Seema Zargar. Spectroscopic and molecular modeling studies of binding interaction between bovine serum albumin and roflumilast.
Drug design, development and therapy.
2018; 12(?):2627-2634. doi:
10.2147/dddt.s169697
. [PMID: 30214151] - J Mokry, A Urbanova, I Medvedova, M Kertys, P Mikolka, P Kosutova, D Mokra. Effects of tadalafil (PDE5 inhibitor) and roflumilast (PDE4 inhibitor) on airway reactivity and markers of inflammation in ovalbumin-induced airway hyperresponsiveness in guinea pigs.
Journal of physiology and pharmacology : an official journal of the Polish Physiological Society.
2017 Oct; 68(5):721-730. doi:
"
. [PMID: 29375047] - Qian Li, Yiya Wang, Lingye Liu, Pengcheng Ma, Li Ding. Pharmacokinetics of Roflumilast and Its Active Metabolite Roflumilast N-Oxide in Healthy Chinese Subjects After Single and Multiple Oral Doses.
European journal of drug metabolism and pharmacokinetics.
2017 Jun; 42(3):371-381. doi:
10.1007/s13318-016-0343-4
. [PMID: 27306372] - Ezigbobiara N Umejiego, Yanhua Wang, Mark A Knepper, Chung-Lin Chou. Roflumilast and aquaporin-2 regulation in rat renal inner medullary collecting duct.
Physiological reports.
2017 Jan; 5(2):. doi:
10.14814/phy2.13121
. [PMID: 28108651] - Omer Uslukaya, Ahmet Turkoglu, Umit Can Yazgan, Ibrahim Kaplan, Ibrahim Ibiloglu, Murat Kapan, Metehan Gumus. The effects of roflumilast on the pancreas and remote organs in a cerulein-induced experimental acute pancreatitis model in rats.
Surgery today.
2016 Dec; 46(12):1435-1442. doi:
10.1007/s00595-016-1329-1
. [PMID: 26983712] - Xinge Cui, Jie Huang, Xin Zheng, Ji Jiang, Yun Kuang, Pei Hu. Simultaneous determination of roflumilast and its metabolite in human plasma by LC-MS/MS: Application for a pharmacokinetic study.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2016 Sep; 1029-1030(?):60-67. doi:
10.1016/j.jchromb.2016.06.001
. [PMID: 27423044] - S Sugin Lal Jabaris, Haridass Sumathy, Ramesh Girish, Shridhar Narayanan, Mani Sugumar, Chidambaram Saravana Babu, Sadagopan Thanikachalam, Mohan Thanikachalam. Phosphodiesterase-4 inhibitors ameliorates cognitive deficits in deoxycorticosterone acetate induced hypertensive rats via cAMP/CREB signaling system.
Brain research.
2015 Oct; 1622(?):279-91. doi:
10.1016/j.brainres.2015.07.003
. [PMID: 26168894] - Sobhana George Sugin Lal Jabaris, Haridass Sumathy, Ramadass Satiesh Kumar, Shridhar Narayanan, Sadagopan Thanikachalam, Chidambaram Saravana Babu. Effects of rolipram and roflumilast, phosphodiesterase-4 inhibitors, on hypertension-induced defects in memory function in rats.
European journal of pharmacology.
2015 Jan; 746(?):138-47. doi:
10.1016/j.ejphar.2014.10.039
. [PMID: 25446433] - Javier Milara, Esteban Morcillo, Daniel Monleon, Herman Tenor, Julio Cortijo. Roflumilast Prevents the Metabolic Effects of Bleomycin-Induced Fibrosis in a Murine Model.
PloS one.
2015; 10(7):e0133453. doi:
10.1371/journal.pone.0133453
. [PMID: 26192616] - Sandro Boland, Jo Alen, Arnaud Bourin, Karolien Castermans, Nicki Boumans, Laura Panitti, Jessica Vanormelingen, Dirk Leysen, Olivier Defert. Novel Roflumilast analogs as soft PDE4 inhibitors.
Bioorganic & medicinal chemistry letters.
2014 Sep; 24(18):4594-4597. doi:
10.1016/j.bmcl.2014.07.016
. [PMID: 25149511] - Kulbhushan Tikoo, Saritha Lodea, Pinakin Arun Karpe, Sandeep Kumar. Calorie restriction mimicking effects of roflumilast prevents diabetic nephropathy.
Biochemical and biophysical research communications.
2014 Aug; 450(4):1581-6. doi:
10.1016/j.bbrc.2014.07.039
. [PMID: 25035926] - Gezim Lahu, Axel Facius. Application of population pharmacokinetic modeling to explore the impact of alternative roflumilast dosing regimens on tolerability.
International journal of clinical pharmacology and therapeutics.
2013 Nov; 51(11):832-6. doi:
10.5414/cp201906
. [PMID: 24152603] - Peng Zhao, Shang-Ke Chen, Ying-Hong Cai, Xiao Lu, Zhe Li, Yuen-Kit Cheng, Cuixian Zhang, Xiaopeng Hu, Xixin He, Hai-Bin Luo. The molecular basis for the inhibition of phosphodiesterase-4D by three natural resveratrol analogs. Isolation, molecular docking, molecular dynamics simulations, binding free energy, and bioassay.
Biochimica et biophysica acta.
2013 Oct; 1834(10):2089-96. doi:
10.1016/j.bbapap.2013.07.004
. [PMID: 23871879] - Mario Thevis, Oliver Krug, Wilhelm Schänzer. Monitoring phosphodiesterase-4 inhibitors using liquid chromatography/(tandem) mass spectrometry in sports drug testing.
Rapid communications in mass spectrometry : RCM.
2013 May; 27(9):993-1004. doi:
10.1002/rcm.6539
. [PMID: 23592202] - Osamu Suzuki, Kiyoshi Mizukami, Maki Etori, Yoshitaka Sogawa, Nana Takagi, Hiroshi Tsuchida, Kiyoshi Morimoto, Taiji Goto, Toshiharu Yoshino, Tsuyoshi Mikkaichi, Kazuki Hirahara, Satoshi Nakamura, Hiroaki Maeda. Evaluation of the therapeutic index of a novel phosphodiesterase 4B-selective inhibitor over phosphodiesterase 4D in mice.
Journal of pharmacological sciences.
2013; 123(3):219-26. doi:
10.1254/jphs.13103fp
. [PMID: 24152964] - Satheeshmanikandan R S Thappali, Kanthikiran V S Varanasi, Sridhar Veeraraghavan, Swaroop Kumar V S Vakkalanka, K Mukkanti. Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study.
Journal of mass spectrometry : JMS.
2012 Dec; 47(12):1612-9. doi:
10.1002/jms.3103
. [PMID: 23280750] - S Vollert, N Kaessner, A Heuser, G Hanauer, A Dieckmann, D Knaack, H P Kley, R Beume, C Weiss-Haljiti. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice.
Diabetologia.
2012 Oct; 55(10):2779-2788. doi:
10.1007/s00125-012-2632-z
. [PMID: 22790061] - Yifei Zhong, Yingwei Wu, Ruijie Liu, Yueyi Deng, Sandeep K Mallipattu, Paul E Klotman, Peter Y Chuang, John C He. Roflumilast enhances the renal protective effects of retinoids in an HIV-1 transgenic mouse model of rapidly progressive renal failure.
Kidney international.
2012 May; 81(9):856-64. doi:
10.1038/ki.2011.467
. [PMID: 22258322] - Patricio E Ray. Can we cure HIV-1-associated nephropathy in transgenic mice?.
Kidney international.
2012 May; 81(9):811-3. doi:
10.1038/ki.2012.13
. [PMID: 22499139] - Shang-Ke Chen, Peng Zhao, Yong-Xian Shao, Zhe Li, Cuixian Zhang, Peiqing Liu, Xixin He, Hai-Bin Luo, Xiaopeng Hu. Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.
Bioorganic & medicinal chemistry letters.
2012 May; 22(9):3261-4. doi:
10.1016/j.bmcl.2012.03.026
. [PMID: 22483586] - Norbert G Knebel, Rolf Herzog, Felix Reutter, Karl Zech. Sensitive quantification of roflumilast and roflumilast N-oxide in human plasma by LC-MS/MS employing parallel chromatography and electrospray ionisation.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2012 Apr; 893-894(?):82-91. doi:
10.1016/j.jchromb.2012.02.038
. [PMID: 22425388] - Gabriel Eckermann, Gezim Lahu, Nassr Nassr, Thomas D Bethke. Absence of pharmacokinetic interaction between roflumilast and digoxin in healthy adults.
Journal of clinical pharmacology.
2012 Feb; 52(2):251-7. doi:
10.1177/0091270010389467
. [PMID: 21257799] - T D Bethke, M Hartmann, A Hünnemeyer, G Lahu, C H Gleiter. Influence of renal impairment on the pharmacokinetics of oral roflumilast: an open-label, parallel-group, single-center study.
International journal of clinical pharmacology and therapeutics.
2011 Aug; 49(8):491-9. doi:
10.5414/cp201556
. [PMID: 21781649] - G Böhmer, C H Gleiter, A Hünnemeyer, G Lahu, T D Bethke. Study investigating pharmacokinetic interaction between theophylline and roflumilast in healthy adults.
International journal of clinical pharmacology and therapeutics.
2011 Jul; 49(7):451-60. doi:
10.5414/cp201535
. [PMID: 21726496] - Christian de Mey, Nassr Nassr, Gezim Lahu. No relevant cardiac, pharmacokinetic or safety interactions between roflumilast and inhaled formoterol in healthy subjects: an open-label, randomised, actively controlled study.
BMC clinical pharmacology.
2011 Jun; 11(?):7. doi:
10.1186/1472-6904-11-7
. [PMID: 21631929] - N McCracken, G Lahu, T D Bethke. Lack of pharmacokinetic and pharmacodynamic interactions of roflumilast with (R, S)-warfarin in healthy adult subjects.
International journal of clinical pharmacology and therapeutics.
2011 Jun; 49(6):388-96. doi:
10.5414/cp201523
. [PMID: 21612746] - Gabriele M Böhmer, Christoph H Gleiter, Klaus Mörike, Nassr Nassr, Antje Walz, Gezim Lahu. No dose adjustment on coadministration of the PDE4 inhibitor roflumilast with a weak CYP3A, CYP1A2, and CYP2C19 inhibitor: an investigation using cimetidine.
Journal of clinical pharmacology.
2011 Apr; 51(4):594-602. doi:
10.1177/0091270010368282
. [PMID: 20484614] - T D Bethke, G Lahu. High absolute bioavailability of the new oral phosphodiesterase-4 inhibitor roflumilast.
International journal of clinical pharmacology and therapeutics.
2011 Jan; 49(1):51-7. doi:
10.5414/cpp49051
. [PMID: 21176727] - Gezim Lahu, Andreas Hünnemeyer, Edgar Diletti, Martin Elmlinger, Peter Ruth, Karl Zech, Nigel McCracken, Axel Facius. Population pharmacokinetic modelling of roflumilast and roflumilast N-oxide by total phosphodiesterase-4 inhibitory activity and development of a population pharmacodynamic-adverse event model.
Clinical pharmacokinetics.
2010 Sep; 49(9):589-606. doi:
10.2165/11536600-000000000-00000
. [PMID: 20690782] - Thomas M Ehrman, David J Barlow, Peter J Hylands. In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Bioorganic & medicinal chemistry.
2010 Mar; 18(6):2204-2218. doi:
10.1016/j.bmc.2010.01.070
. [PMID: 20188577] - Nassr Nassr, Andreas Huennemeyer, Rolf Herzog, Oliver von Richter, Robert Hermann, Manuela Koch, Kevin Duffy, Karl Zech, Gezim Lahu. Effects of rifampicin on the pharmacokinetics of roflumilast and roflumilast N-oxide in healthy subjects.
British journal of clinical pharmacology.
2009 Oct; 68(4):580-7. doi:
10.1111/j.1365-2125.2009.03478.x
. [PMID: 19843061] - J Cortijo, A Iranzo, X Milara, M Mata, M Cerdá-Nicolás, A Ruiz-Saurí, H Tenor, A Hatzelmann, E J Morcillo. Roflumilast, a phosphodiesterase 4 inhibitor, alleviates bleomycin-induced lung injury.
British journal of pharmacology.
2009 Feb; 156(3):534-44. doi:
10.1111/j.1476-5381.2008.00041.x
. [PMID: 19154443] - Kathleen A Neville, Stanley J Szefler, Susan M Abdel-Rahman, Gezim Lahu, Karl Zech, Rolf Herzog, Thomas D Bethke, Melanie C Gleason, Gregory L Kearns. Single-dose pharmacokinetics of roflumilast in children and adolescents.
Journal of clinical pharmacology.
2008 Aug; 48(8):978-85. doi:
10.1177/0091270008319466
. [PMID: 18508947] - Robert Hermann, Werner Siegmund, Thomas Giessmann, Kristin Westphal, Anita Weinbrenner, Bernhard Hauns, Felix Reutter, Gezim Lahu, Karl Zech, Thomas D Bethke. The oral, once-daily phosphodiesterase 4 inhibitor roflumilast lacks relevant pharmacokinetic interactions with inhaled budesonide.
Journal of clinical pharmacology.
2007 Aug; 47(8):1005-13. doi:
10.1177/0091270007300950
. [PMID: 17660483] - Robert Hermann, Nassr Nassr, Gezim Lahu, Eva Péterfai, Dietrich Knoerzer, Rolf Herzog, Karl Zech, Christian de Mey. Steady-state pharmacokinetics of roflumilast and roflumilast N-oxide in patients with mild and moderate liver cirrhosis.
Clinical pharmacokinetics.
2007; 46(5):403-16. doi:
10.2165/00003088-200746050-00003
. [PMID: 17465639] - Oliver von Richter, Gezim Lahu, Andreas Huennemeyer, Rolf Herzog, Karl Zech, Robert Hermann. Effect of fluvoxamine on the pharmacokinetics of roflumilast and roflumilast N-oxide.
Clinical pharmacokinetics.
2007; 46(7):613-22. doi:
10.2165/00003088-200746070-00006
. [PMID: 17596106] - T D Bethke, T Giessmann, K Westphal, A Weinbrenner, B Hauns, D Hauschke, M David, G Lahu, K Zech, R Hermann, W Siegmund. Roflumilast, a once-daily oral phosphodiesterase 4 inhibitor, lacks relevant pharmacokinetic interactions with inhaled salbutamol when co-administered in healthy subjects.
International journal of clinical pharmacology and therapeutics.
2006 Nov; 44(11):572-9. doi:
10.5414/cpp44572
. [PMID: 17176624] - Kerryn McCluskie, Uwe Klein, Chris Linnevers, Yu-Hua Ji, Alfred Yang, Craig Husfeld, G Roger Thomas. Phosphodiesterase type 4 inhibitors cause proinflammatory effects in vivo.
The Journal of pharmacology and experimental therapeutics.
2006 Oct; 319(1):468-76. doi:
10.1124/jpet.106.105080
. [PMID: 16861399] - Ellena J Growcott, Karen G Spink, Xiaohui Ren, Saliha Afzal, Kathy H Banner, John Wharton. Phosphodiesterase type 4 expression and anti-proliferative effects in human pulmonary artery smooth muscle cells.
Respiratory research.
2006 Jan; 7(?):9. doi:
10.1186/1465-9921-7-9
. [PMID: 16423283] - Zheng Huang, Joseph A Mancini. Phosphodiesterase 4 inhibitors for the treatment of asthma and COPD.
Current medicinal chemistry.
2006; 13(27):3253-62. doi:
10.2174/092986706778773040
. [PMID: 17168849] - Hyun Jeong Kwak, Jin Sook Song, Jun Young Heo, Sung Don Yang, Ji-Youn Nam, Hyae Gyeong Cheon. Roflumilast inhibits lipopolysaccharide-induced inflammatory mediators via suppression of nuclear factor-kappaB, p38 mitogen-activated protein kinase, and c-Jun NH2-terminal kinase activation.
The Journal of pharmacology and experimental therapeutics.
2005 Dec; 315(3):1188-95. doi:
10.1124/jpet.105.092056
. [PMID: 16126838] - Antonio Maurizio Vignola. PDE4 inhibitors in COPD--a more selective approach to treatment.
Respiratory medicine.
2004 Jun; 98(6):495-503. doi:
10.1016/j.rmed.2003.12.012
. [PMID: 15191033] - Regina Draheim, Ute Egerland, Chris Rundfeldt. Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations.
The Journal of pharmacology and experimental therapeutics.
2004 Feb; 308(2):555-63. doi:
10.1124/jpet.103.059097
. [PMID: 14610230]