生物活性

• 靶点	COX2 IC50:30nM

• 描述Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively^[3]. Carprofen (10 µg/mL) shows cytoprotective effects in CCL (cranial) and CaCL (caudal) cells and decreases apoptosis of both cells. Carprofen (10 μg/mL) had the greatest cytoprotective effects for CCL and CaCL cells^[4]. Carprofen acts in vivo on target tissues as COX-1-sparing drugs by sparing gastric PGE1 and PGE2 synthesis and production of TXB2 (thromboxane B2) by platelets^[5]. The administration of maropitant alone and carprofen alone produced clinically significant sparing effects on the sevoflurane MAC-BAR (minimum alveolar concentration for blunting adrenergic response) in dogs. However, the combination of maropitant and carprofen did not produce any additive effect on the sevoflurane MAC-BAR reduction^[6].
• 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
  NCT01448785	Obesity Morbi... more >>d Obesity Collapse <<	Not Applicable	Unknown	January 2015	France ... more >> Polyclinique de Rillieux, Clinique Lyon-Nord Recruiting RILLIEUX Cedex, France, 69165 Contact: Jerome Dargent, MD          Principal Investigator: Jerome Dargent, MD          Germany MIC Ev. Krankenhaus Hubertus Recruiting Berlin, Germany, 14129 Contact: Martin Susewind, MD          Principal Investigator: Martin Susewind, MD          SRH Wald-Klinikum Gera Recruiting Gera, Germany, 07548 Contact: Christine Stroh, MD          Principal Investigator: Christine Stroh, MD          Wolfart Klinik Active, not recruiting Graefelfing, Germany, 92166 Universitätsklinikum Hamburg-Eppendorf Recruiting Hamburg, Germany, 20246 Contact: Oliver Mann, MD          Principal Investigator: Oliver Mann, MD          Stadtkrankenhaus Schwabach Recruiting Schwabach, Germany, 91126 Contact: Thomas Horbach, MD          Principal Investigator: Thomas Horbach, MD          Italy Azienda Ospedaliera- University Not yet recruiting Pisa, Italy Contact: Marco Anselmino, MD          Principal Investigator: Marco Anselmino, MD          Clinica San Luca Torino Not yet recruiting Turin, Italy Contact: Giuseppe M Rovera, MD          Principal Investigator: Giuseppe M Rovera, MD          Vicenza Regional Hospital Not yet recruiting Vicenza, Italy, 36100 Contact: Franco Favretti, MD          Principal Investigator: Franco Favretti, MD          Spain Complutense University of Madrid Hospital Clinico "San Carlos" Not yet recruiting Madrid, Spain, 28290 Contact: Antonio J Torres, MD          Principal Investigator: Antonio J Torres, MD          Hospital Virgen del Roció Recruiting Sevilla, Spain, 41013 Contact: Salvador Morales Conde, MD          Principal Investigator: Salvador Morales Conde, MD          Switzerland Klinik Lindberg Recruiting Winterthur, Switzerland, 8400 Contact: Fritz Horber, MD          Principal Investigator: Fritz Horber, MD          United Kingdom Spire Southampton Hospital Not yet recruiting Hampshire, Southampton, United Kingdom, SO16 6UY Contact: James Byrne, MD          Principal Investigator: James Byrne, MD          St. Anthony's Hospital Not yet recruiting North Cheam, Surrey, United Kingdom, SM3 9DW Contact: Alberic Fiennes, MD          Principal Investigator: Alberic Fiennes, MD          Mid Yorkshire NHS Trust Not yet recruiting Dewsbury, West Yorkshire, United Kingdom, WF13 4HS Contact: Chinnadorai Rajeswaran, MD          Principal Investigator: Chinnadorai Rajeswaran, MD Collapse <<

• 参考文献

• [1] Bialer M, Johannessen SI, et al. Progress report on new antiepileptic drugs: a summary of the Seventh Eilat Conference (EILAT VII). Epilepsy Res. 2004 Sep-Oct;61(1-3):1-48.

  [2] Ricketts AP, Lundy KM, Seibel SB. Evaluation of selective inhibition of canine cyclooxygenase 1 and 2 by carprofen and other nonsteroidal anti-inflammatory drugs. Am J Vet Res. 1998 Nov;59(11):1441-6.

  [3] Favia AD, Habrant D, Scarpelli R, et al. Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor. J Med Chem. 2012;55(20):8807-8826

  [4] Waldherr K, Zurbriggen A, Spreng DE, Forterre S. In vitro cytoprotective effects of acetylsalicylic acid, carprofen, meloxicam, or robenacoxib against apoptosis induced by sodium nitroprusside in canine cruciate ligament cells. Am J Vet Res. 2012;73(11):1752-1758

  [5] Sessions JK, Reynolds LR, Budsberg SC. In vivo effects of carprofen, deracoxib, and etodolac on prostanoid production in blood, gastric mucosa, and synovial fluid in dogs with chronic osteoarthritis. Am J Vet Res. 2005;66(5):812-817

  [6] Fukui S, Ooyama N, Tamura J, et al. Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs. J Vet Med Sci. 2017;79(3):502-508

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