Anagrelide (BioDeep_00000018449)

   

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-, monohydrochloride

化学式: C10H7Cl2N3O (254.99661519999998)
中文名称: 阿那格雷
谱图信息: 最多检出来源 Danio rerio(blood) 20%

分子结构信息

SMILES: C1C2=C(C=CC(=C2Cl)Cl)N=C3N1CC(=O)N3
InChI: InChI=1S/C10H7Cl2N3O/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7/h1-2H,3-4H2,(H,13,14,16)

描述信息

Anagrelide is only found in individuals that have used or taken this drug. It is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia. [Wikipedia]The mechanism by which anagrelide reduces blood platelet count is still under investigation. Studies in patients support a hypothesis of dose-related reduction in platelet production resulting from a decrease in megakaryocyte hypermaturation. In blood withdrawn from normal volunteers treated with anagrelide, a disruption was found in the postmitotic phase of megakaryocyte development and a reduction in megakaryocyte size and ploidy. At therapeutic doses, anagrelide does not produce significant changes in white cell counts or coagulation parameters, and may have a small, but clinically insignificant effect on red cell parameters. Anagrelide inhibits cyclic AMP phosphodiesterase III (PDEIII). PDEIII inhibitors can also inhibit platelet aggregation. However, significant inhibition of platelet aggregation is observed only at doses of anagrelide higher than those required to reduce platelet count.
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents
C78275 - Agent Affecting Blood or Body Fluid > C1327 - Antiplatelet Agent
D006401 - Hematologic Agents > D010975 - Platelet Aggregation Inhibitors
D006401 - Hematologic Agents > D005343 - Fibrinolytic Agents
D050299 - Fibrin Modulating Agents
D002317 - Cardiovascular Agents

同义名列表

10 个代谢物同义名

Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-, monohydrochloride; 6,7-Dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3H)-one hydrochloride; 6,7-dichloro-1H,2H,3H,5H-imidazolidino[2,1-b]quinazolin-2-one; Anagrelide hydrochloride; Anagrelidum; anagrelide; Anagrelida; BL-4162a; Agrelin; Agrylin



数据库引用编号

10 个数据库交叉引用编号

分类词条

相关代谢途径

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代谢反应

0 个相关的代谢反应过程信息。

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Plant Reactome(0)

INOH(0)

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1 个相关的物种来源信息

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  • 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。

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文献列表

  • Jacek Kwiatkowski, Małgorzata Kuliszkiewicz-Janus, Weronika Rymer, Bożena Jaźwiec, Rafał Małecki. Treatment of Essential Thrombocythemia with Anagrelide Is Associated with an Increased Risk of Worsened Kidney Function. Pharmacology. 2021; 106(5-6):316-322. doi: 10.1159/000513377. [PMID: 33691325]
  • Ivan Krečak, Marko Lucijanić. Modifying the Effects of Cytoreductive Drugs on Kidney Function in Myeloproliferative Neoplasms. Pharmacology. 2021; 106(7-8):451-452. doi: 10.1159/000516894. [PMID: 34139702]
  • M I A Abdel Maksoud, Gharieb S El-Sayyad, A H Ashour, Ahmed I El-Batal, Mahmmoud S Abd-Elmonem, Hassan A M Hendawy, E K Abdel-Khalek, Sh Labib, E Abdeltwab, M M El-Okr. Synthesis and characterization of metals-substituted cobalt ferrite [Mx Co(1-x) Fe2O4; (M = Zn, Cu and Mn; x = 0 and 0.5)] nanoparticles as antimicrobial agents and sensors for Anagrelide determination in biological samples. Materials science & engineering. C, Materials for biological applications. 2018 Nov; 92(?):644-656. doi: 10.1016/j.msec.2018.07.007. [PMID: 30184791]
  • Petro E Petrides, Christian Schoergenhofer, Rudolf Widmann, Bernd Jilma, Christoph S Klade. Pharmacokinetics of a Novel Anagrelide Extended-Release Formulation in Healthy Subjects: Food Intake and Comparison With a Reference Product. Clinical pharmacology in drug development. 2018 02; 7(2):123-131. doi: 10.1002/cpdd.340. [PMID: 28301098]
  • Manuel Martínez-Sellés, Tomás Datino, Lourdes Figueiras-Graillet, Joubert G Gama, Christopher Jones, Richard Franklin, Francisco Fernández-Avilés. Cardiovascular safety of anagrelide in healthy subjects: effects of caffeine and food intake on pharmacokinetics and adverse reactions. Clinical drug investigation. 2013 Jan; 33(1):45-54. doi: 10.1007/s40261-012-0032-2. [PMID: 23184666]
  • Carlos Besses, Wolfgang Zeller, Alberto Alvarez-Larrán, Ruth Coll, Steven Troy, Jaideep Purkayastha, Patrick Martin, Christian Freitag. Pharmacokinetics and tolerability of anagrelide hydrochloride in young (18 - 50 years) and elderly (≥ 65 years) patients with essential thrombocythemia. International journal of clinical pharmacology and therapeutics. 2012 Nov; 50(11):787-96. doi: 10.5414/cp201711. [PMID: 22943924]
  • Itsuro Kazama, Yasuhiro Endo, Hiroaki Toyama, Yutaka Ejima, Shin Kurosawa, Yoshimichi Murata, Mitsunobu Matsubara, Yoshio Maruyama. Compensatory thrombopoietin production from the liver and bone marrow stimulates thrombopoiesis of living rat megakaryocytes in chronic renal failure. Nephron extra. 2011 Jan; 1(1):147-56. doi: 10.1159/000333018. [PMID: 22470388]
  • Jacek Treliński, Agnieszka Wierzbowska, Anna Krawczyńska, Agata Sakowicz, Tadeusz Pietrucha, Piotr Smolewski, Tadeusz Robak, Krzysztof Chojnowski. Plasma levels of angiogenic factors and circulating endothelial cells in essential thrombocythemia: correlation with cytoreductive therapy and JAK2-V617F mutational status. Leukemia & lymphoma. 2010 Sep; 51(9):1727-33. doi: 10.3109/10428194.2010.500435. [PMID: 20615083]
  • Maria do Carmo Filomena Mesquita, Eugénie Bakoto Sol, Marianne Malarme, Denis Noubouossie, Anne Claire Demulder. Management of refractory essential thrombocythemia with anagrelide in a patient undergoing hemodialysis. Clinical therapeutics. 2009 Nov; 31(11):2559-64. doi: 10.1016/j.clinthera.2009.11.006. [PMID: 20110000]
  • Petro E Petrides, Heinz Gisslinger, Michael Steurer, Werner Linkesch, Günther Krumpl, Agnes Schüller, Rudolf Widmann. Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation. Clinical therapeutics. 2009 Feb; 31(2):386-98. doi: 10.1016/j.clinthera.2009.02.008. [PMID: 19302911]
  • Jan Palmblad, Magnus Björkholm, Jack Kutti, Gerd Lärfars, Eva Löfvenberg, Berit Markevärn, Mats Merup, Nils Mauritzson, Jan Westin, Jan Samuelsson, Gunnar Birgegård. TPO, but not soluble-IL-6 receptor, levels increase after anagrelide treatment of thrombocythemia in chronic myeloproliferative disorders. International journal of medical sciences. 2008 Apr; 5(2):87-91. doi: 10.7150/ijms.5.87. [PMID: 18414650]
  • Keyvan Rezaï, François Lokiec, Isabelle Grandjean, Sophie Weill, Patricia de Cremoux, Vincent Bordier, Richard Ekue, Mickael Garcia, Marie-France Poupon, Didier Decaudin. Impact of imatinib on the pharmacokinetics and in vivo efficacy of etoposide and/or ifosfamide. BMC pharmacology. 2007 Oct; 7(?):13. doi: 10.1186/1471-2210-7-13. [PMID: 17963518]
  • Jan Jacques Michiels, Zwi Berneman, Wilfried Schroyens, Peter J Koudstaal, Jan Lindemans, H A Martino Neumann, Huub H D M van Vliet. Platelet-mediated erythromelalgic, cerebral, ocular and coronary microvascular ischemic and thrombotic manifestations in patients with essential thrombocythemia and polycythemia vera: a distinct aspirin-responsive and coumadin-resistant arterial thrombophilia. Platelets. 2006 Dec; 17(8):528-44. doi: 10.1080/09537100600758677. [PMID: 17127481]
  • Rosana F Marta, Nora P Goette, Felisa C Molinas. [Megakaryopoietic cytokine levels in patients with essential thrombocythemia and their relationship with clinical and biochemical features]. Medicina. 2006; 66(6):540-6. doi: NULL. [PMID: 17240625]
  • Z Zhu, R Gonthier, L Neirinck. High-performance liquid chromatography-mass spectrometry method for determination of anagrelide in human plasma. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2005 Aug; 822(1-2):238-43. doi: 10.1016/j.jchromb.2005.06.021. [PMID: 16005692]
  • Björn Andreasson, Eva Löfvenberg, Jan Westin. Management of patients with polycythaemia vera: results of a survey among Swedish haematologists. European journal of haematology. 2005 Jun; 74(6):489-95. doi: 10.1111/j.1600-0609.2005.00424.x. [PMID: 15876252]
  • Graham E J Rodwell, Megan L Troxell, Richard A Lafayette. Renal tubular injury associated with anagrelide use. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association. 2005 May; 20(5):988-90. doi: 10.1093/ndt/gfh726. [PMID: 15728271]
  • Yesid Alvarado, Jorge Cortes, Srdan Verstovsek, Deborah Thomas, Stephan Faderl, Zeev Estrov, Hagop Kantarjian, Francis J Giles. Pilot study of pegylated interferon-alpha 2b in patients with essential thrombocythemia. Cancer chemotherapy and pharmacology. 2003 Jan; 51(1):81-6. doi: 10.1007/s00280-002-0533-4. [PMID: 12497210]
  • P R Lev, R F Marta, P Vassallu, F C Molinas. Variation of PDGF, TGFbeta, and bFGF levels in essential thrombocythemia patients treated with anagrelide. American journal of hematology. 2002 Jun; 70(2):85-91. doi: 10.1002/ajh.10091. [PMID: 12111780]
  • Michael B Streiff, Brad Smith, Jerry L Spivak. The diagnosis and management of polycythemia vera in the era since the Polycythemia Vera Study Group: a survey of American Society of Hematology members' practice patterns. Blood. 2002 Feb; 99(4):1144-9. doi: 10.1182/blood.v99.4.1144. [PMID: 11830459]
  • H S Gilbert. Diagnosis and treatment of thrombocythemia in myeloproliferative disorders. Oncology (Williston Park, N.Y.). 2001 Aug; 15(8):989-96, 998; discussion 999. doi: NULL. [PMID: 11548978]
  • S L Pescatore, C Lindley. Anagrelide: a novel agent for the treatment of myeloproliferative disorders. Expert opinion on pharmacotherapy. 2000 Mar; 1(3):537-46. doi: 10.1517/14656566.1.3.537. [PMID: 11249536]
  • M D Oertel. Anagrelide, a selective thrombocytopenic agent. American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists. 1998 Oct; 55(19):1979-86. doi: 10.1093/ajhp/55.19.1979. [PMID: 9784784]
  • N A Meanwell, R D Dennis, H R Roth, M J Rosenfeld, E C Smith, J J Wright, J O Buchanan, C L Brassard, M Gamberdella, E Gillespie. Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility. Journal of medicinal chemistry. 1992 Jul; 35(14):2688-96. doi: 10.1021/jm00092a020. [PMID: 1321911]
  • E M Mazur, A G Rosmarin, P A Sohl, J L Newton, A Narendran. Analysis of the mechanism of anagrelide-induced thrombocytopenia in humans. Blood. 1992 Apr; 79(8):1931-7. doi: NULL. [PMID: 1562721]
  • S Seiler, A J Arnold, R I Grove, C A Fifer, S L Keely, H C Stanton. Effects of anagrelide on platelet cAMP levels, cAMP-dependent protein kinase and thrombin-induced Ca++ fluxes. The Journal of pharmacology and experimental therapeutics. 1987 Nov; 243(2):767-74. doi: NULL. [PMID: 2824759]
  • E H Kerns, J W Russell, D G Gallo. Determination of anagrelide in plasma by capillary gas chromatography-mass spectrometry. Journal of chromatography. 1987 May; 416(2):357-64. doi: 10.1016/0378-4347(87)80520-0. [PMID: 3611267]
  • C R Benedict, B Mathew, K A Rex, J Cartwright, L A Sordahl. Correlation of plasma serotonin changes with platelet aggregation in an in vivo dog model of spontaneous occlusive coronary thrombus formation. Circulation research. 1986 Jan; 58(1):58-67. doi: 10.1161/01.res.58.1.58. [PMID: 3943156]
  • W F Clark, G J Tevaarwerk, T A Moriarity, B D Reid. Inhibitors of immune complex induced human platelet aggregation and release in plasma. Thrombosis research. 1982 Dec; 28(5):681-8. doi: 10.1016/0049-3848(82)90159-1. [PMID: 7167877]
  • R C Gaver, G Deeb, K A Pittman, R D Smyth. Disposition of anagrelide, an inhibitor of platelet aggregation. Clinical pharmacology and therapeutics. 1981 Mar; 29(3):381-6. doi: 10.1038/clpt.1981.52. [PMID: 7471608]