生物活性

• 靶点

  COX1 IC50:0.5μM

  COX2 IC50:2.33μM

• 描述Cyclooxygenase (COX) is the rate-limiting enzyme for the synthesis of prostaglandins. Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits both COX1 and COX2 in blood with the IC₅₀ values of 0.11 μM and 0.88 μM, respectively^[1]. Ketoprofen inhibited thromboxane B₂ (T_xB₂) production in freshly isolated platelets from human blood with an IC₅₀ value of 7.4 μM. The efficacy of ketoprofen in inhibiting LPS-induced T_xB₂ production in human mononuclear cells was determined with an IC₅₀ value of 7.7 μM^[2]. When HaCaT cells were irradiated with UVB (10 mJ/cm²), the activity of caspase-3 and the number of cells at the G2 phase were significant increased compared to cells without ketoprofen treatment. It was also shown that 100 μM Ketoprofen significantly provoked the accumulation of cyclin B1-cdc2-p21 complexes, as well as the amounts of Tyr15-phosphorylated cdc2 and p21 protein^[3].
• 作用机制Ketoprofen inhibits the activity of cyclooxygenase by conjugating with glucuronide and with coenzyme A^[4].

• 动物研究
  剂量	Dog: 0.5 mg/kg - 2 mg/kg[5] (s.c.); 0.25 mg/kg - 5 mg/kg[5] (p.o.) Rat: 50 mg/kg[6] (p.o.)
  给药途径	s.c., p.o.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01307020	Pain	Phase 2	Completed	-	Germany ... more >> Klinik und Polickinik für Mund-Kiefer-Gesichtschirurgie/Plastische Operationen Greifswald Greifswald, Mecklenburg-Vorpommern, Germany, 17475 Klinik für Mund-, Kiefer- und Gesichtschirurgie, Universitätsklinikum Schleswig Holstein, Campus Kiel Kiel, Schleswig-Holstein, Germany, 24105 Hungary Dr Tóth Bagi Zoltán Fogászati Rendeloje Budapest, Hungary, 1052 Italy Centro di Farmacologia Clinica per la Sperimentazione dei Farmaci Pisa, Italy, 56126 Centro di Ricerche Cliniche di Verona Srl. Policlinico G.B.Rossi Verona, Italy, 37134 Poland Gabinet Stomatologiczny Andrzej Wojtowicz AW Clinic Warsaw, Mazowieckie, Poland, 00-852 Dental Service spólka jawna Warszawa, Mazowieckie, Poland, 02-791 Spain Hospital Médico Quirúrgico de Conxo Santiago de Compostela, A Coruña, Spain, 15706 Facultad de Odontología. Departamento de Cirugía Bucal y Maxilofacial, University of Barcelona - Bellvitge Institute for Biomedical Research (IDIBELL) L'Hospitalet de Llobregat, Barcelona, Spain, 08907 Universidad Complutense de Madrid Madrid, Spain, 28040 Departamento de Estomatología, Facultad de Odontología. Universidad de Sevilla Sevilla, Spain, 41009 Departament d'Estomatologia, Clínica Odontològica, Universidad de Valencia - Fundació Lluís Alcanyís Valencia, Spain, 046010 Hospital General Universitario de Valencia Valencia, Spain, 46014 United Kingdom The School of Dentistry, College of Medical and Dental Sciences, University of Birmingham Birmingham, England, United Kingdom, B4 6 NN University Dental School Manchester Manchester, England, United Kingdom, M15 6FH University Dental Hospital Cardiff, Wales, United Kingdom, CF14 4 XY Collapse <<
  NCT02092012	Pain	Phase 4	Unknown	July 2014	Turkey ... more >> Erciyes Univercity Medicine Faculty Recruiting Kayseri, Turkey, 38039 Contact: selda kayaaltı, resident    +905558168918    drselda@hotmail.com    Contact: fatih ugur, assoc    +905359730073    ugurf@erciyes.edu.tr Collapse <<
  NCT01307020	-	-	Completed	-	-

• 更多
• 参考文献

• [1] Cryer B, Feldman M. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med. 1998;104(5):413-21.

  [2] Grossman CJ, Wiseman J, et al. Inhibition of constitutive and inducible cyclooxygenase activity in human platelets and mononuclear cells by NSAIDs and Cox 2 inhibitors. Inflamm Res. 1995;44(6):253-7.

  [3] Liu S, Mizu H, et al. Molecular response to phototoxic stress of UVB-irradiated ketoprofen through arresting cell cycle in G2/M phase and inducing apoptosis. Biochem Biophys Res Commun. 2007;364(3):650-5.

  [4] Levoin N, Blondeau C, et al. Elucidation of the mechanism of inhibition of cyclooxygenases by acyl-coenzyme A and acylglucuronic conjugates of ketoprofen. Biochem Pharmacol. 2004;68(10):1957-69.