Trifluoperazine 2HCl

产品说明书

Print
Chemical Structure| 440-17-5 同义名 : 盐酸三氟拉嗪;三氟吡拉嗪;甲哌氟丙嗪;三氟拉嗪二盐酸盐 ;SKF5019; Trazine; Tryptazine dihydrochloride; NSC 17474; TFP; Trifluoperazine(dihydrochloride)
CAS号 : 440-17-5
货号 : A372302
分子式 : C21H26Cl2F3N3S
纯度 : 98%
分子量 : 480.418
MDL号 : MFCD00012656
存储条件:

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(104.08 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(104.08 mM),配合低频超声助溶

动物实验配方:

PO 0.5% CMC-Na 15 mg/mL suspension

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... 展开 >>t Gain Psychotropic Induced Weight Gain 收起 << Phase 1 Unknown May 2011 United States, Ohio ... 展开 >> 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 收起 <<
NCT02600741 - Completed - -
NCT01765829 Psychosis Nos/Other Phase 3 Unknown November 2015 Spain ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.41mL

2.08mL

1.04mL

20.82mL

4.16mL

2.08mL

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