生物活性

• 描述Trifluoperazine dihydrochloride (TFP) is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is also a potent dopamine D2 receptor inhibitor^[3]. Trifluoperazine, as an anxiolytic and antipsychotic agent, has been an extensively studied drug molecule that has been used as a calmodulin inhibitor^[4]. Trifluoperazine and chlorpromazine inhibited in a dose-dependent manner the stimulation of glycogenolysis, gluconeogenesis, and ureogenesis due to alpha 1-adrenergic stimulation in rat hepatocytes. Chlorpromazine and trifluoperazine are much more potent at alpha 1- than at alpha 2-adrenergic receptors^[3]. Larger doses of trifluoperazine (1.125-4.5 mg/kg) totally inhibited apomorphine-induced (0.125 mg/kg, s.c.) stereotypy in both groups^[5].
• 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
  NCT01231074	Obesity Weigh... more >>t Gain Psychotropic Induced Weight Gain Collapse <<	Phase 1	Unknown	May 2011	United States, Ohio ... more >> Nationwide Children's Hospital Recruiting Columbus, Ohio, United States, 43205 Contact: Ihuoma Eneli, MD, MS    614-722-4089    ihuoma.eneli@nationwidechildrens.org    Contact: Mary Ann Murphy, MD, PhD    614-722-2291    maryann.murphy@nationwidechildrens.org Collapse <<
  NCT02600741	-	-	Completed	-	-
  NCT01765829	Psychosis Nos/Other	Phase 3	Unknown	November 2015	Spain ... more >> Mental Health Unit Villamartín Recruiting Villamartín, Cádiz, Spain, 11650 Contact: José María Mongil San Juan, MD    0034956040209    cheman45@gmail.com    Principal Investigator: José María Mongil San Juan, MD          Mental Health Unit Baza Recruiting Baza, Granada, Spain, 18800 Contact: Eva Bravo Barba, MD       eva.bravo.barba@gmail.com    Principal Investigator: Eva Bravo Barba, MD          Mental Health Unit Motril Recruiting Motril, Granada, Spain, 18600 Contact: María Luisa Barrigón Estévez, MD    0034958038849    marial.barrigon.sspa@juntadeandalucia.es    Principal Investigator: María Luisa Barrigón Estévez, MD          Mental Health Unit Andújar Recruiting Andújar, Jaén, Spain, 23740 Contact: Fernando Sarramea Crespo, MD, PhD    0034953021717    fernandosarramea@hotmail.com    Principal Investigator: Farnando Sarramea Crespo, MD, PhD          Mental Health Unit Martos Recruiting Martos, Jaén, Spain, 23600 Contact: Miguel Ortigosa Luque, MD       migueortigosa@hotmail.com    Principal Investigator: Miguel Ortigosa Luque, MD          Mental Health Unit Miraflores Not yet recruiting Alcobendas, Madrid, Spain, 28100 Contact: María Luisa Zamarro Arraz, MD, PhD    0034916530108    zamarroluisa@yahoo.es    Principal Investigator: María Luisa Zamarro Arraz, MD, PhD          Hospital Infanta Sofía Not yet recruiting San Sebastian de los Reyes, Madrid, Spain, 28702 Contact: María Rosario Gutiérrez Labrador, MD       rosagutierrez@psiquiatra.e.telefonica.net    Principal Investigator: María Rosario Guitiérrez Labrador, MD          Mental Health Unit Valle del Guadalhorce Not yet recruiting Cártama, Málaga, Spain, 29580 Contact: Daniel Gutiérrez Castillo, MD    0034951033931    dgutierrezcastillo@gmail.com    Principal Investigator: Daniel Gutiérrez Castillo, MD          Mental Health Unit Las Lagunas Not yet recruiting Fuengiróla, Málaga, Spain, 29650 Contact: María Isabel Osuna Carmona, MD       maribelosunac@hotmail.com    Principal Investigator: María Isabel Osuna Carmona, MD          Fundación Argibide Not yet recruiting Pamplona, Navarra, Spain, 31007 Contact: Ignacio Mata Pastor, MD, PhD    0034948266650    nacho.mata70@gmail.com    Principal Investigator: Ignacio Mata Pastor, MD, PhD          Hospital El Tomillar Recruiting Dos Hermanas, Seville, Spain, 41700 Contact: Joaquín Carlos Martín Muñoz, MD, PhD    0034955016083    joaquinmartin@hotmail.com    Principal Investigator: Joaquín Carlos Martín Muñoz, MD, PhD          Hospital Francesc de Borja Recruiting Gandía, Valencia, Spain, 46700 Contact: María Lacruz Silvestre, MD, PhD       maria.lacruz.silvestre@gmail.com    Principal Investigator: María Lacruz Silvestre, MD, PhD          Hospital de Basurto Not yet recruiting Bilbao, Spain, 48013 Contact: Sonia Bustamante Madariaga, MD, Phd    0034944 006137    sonia.bustamantemadariaga@osakidetza.net    Principal Investigator: Sonia Bustamante Madariaga, MD, PhD          Mental Health Unit Tetuán Not yet recruiting Madrid, Spain, 28003 Contact: Mariano Hernández Monsalve, MD, PhD    0034915347363    hergoico@gmail.com    Contact: Ruth Berdún Pe, MD       ruthberdun@yahoo.es    Principal Investigator: Mariano Hernández Monsalve, MD, PhD          Lafora Hospital Not yet recruiting Madrid, Spain, 28049 Contact: Juan Dios Molina Martín, MD, PhD       jmolinamar@hotmail.com    Principal Investigator: Juan Dios Molina Martín, MD, PhD          Hospital Carlos Haya Recruiting Málaga, Spain, 29009 Contact: Fermín Mayoral Cleríes, Md, PhD       fermin.mayoral.sspa@juntadeandalucia.es    Principal Investigator: Fermín Mayoral Cleríes, MD, PhD          Virgen del Rocío Hospital Recruiting Seville, Spain, 41013 Contact: Clara M. Rosso Fernández, MD    0034955013414    claram.rosso.sspa@juntadeandalucia.es    Contact: Miguel Ruiz Veguilla, MD, PhD    0034955013414    mruizveguilla@yahoo.com    Principal Investigator: Miguel Ruiz Veguilla, MD, PhD Collapse <<

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• 参考文献

• [1] Cahir M, King DJ. Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4.

  [2] Lahti RA, Evans DL, et al. Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur J Pharmacol. 1993 Jun 4;236(3):483-6.

  [3] Huerta-Bahena J, Villalobos-Molina R, García-Sáinz JA. Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects. Mol Pharmacol. 1983;23(1):67‐70

  [4] Howland RH. Trifluoperazine: A Sprightly Old Drug. J Psychosoc Nurs Ment Health Serv. 2016;54(1):20‐22

  [5] Rupniak NM, Boyce S, Jenner P, Marsden CD. Interpretation of changes in apomorphine-induced stereotyped behaviour in rats receiving continuous administration of trifluorperazine for 15 months. Neuropharmacology. 1984;23(8):893‐898

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