货号:A372302
同义名:
盐酸三氟拉嗪;三氟吡拉嗪
/ Trifluoperazine (hydrochloride);SKF5019
Trifluoperazine 2HCl是一种 多巴胺 D2 受体抑制剂,具有抗多巴胺能和抗肾上腺能作用,属于 苯噻嗪 类化合物。
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产品名称 | D1 receptor ↓ ↑ | D2 receptor ↓ ↑ | D3 receptor ↓ ↑ | D4 receptor ↓ ↑ | D5 receptor ↓ ↑ | DAT ↓ ↑ | Dopamine receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Penfluridol |
+
Dopamine receptor, Ki: 1.6 μM |
98% | |||||||||||||||||
Ansofaxine HCl |
++
Dopamine receptor, IC50: 491 nM |
99% | |||||||||||||||||
Tetrahydroberberine,THB |
+
D2 receptor, pKi: 6.08 |
98+% | |||||||||||||||||
Prochlorperazine Maleate | ✔ | 98% (HPLC) | |||||||||||||||||
Olanzapine | ✔ | 99+% | |||||||||||||||||
Trifluoperazine |
++++
Dopamine D2 receptor, IC50: 1.1 nM |
98% | |||||||||||||||||
Ropinirole hydrochloride |
++
D2 receptor, Ki: 29 nM |
99% | |||||||||||||||||
Lurasidone |
++++
D2 receptor, Ki: 1 nM |
98% | |||||||||||||||||
Levosulpiride | ✔ | 99+% | |||||||||||||||||
Pridopidine | ✔ | 95% | |||||||||||||||||
Metoclopramide | ✔ | ✔ | 99+% | ||||||||||||||||
Molindone HCl | ✔ | 99% | |||||||||||||||||
Sulpiride | ✔ | 99+% | |||||||||||||||||
Perospirone |
++++
D2 receptor, Ki: 1.4 nM |
99% | |||||||||||||||||
Perospirone HCl |
++++
D2 receptor, Ki: 1.4 nM |
99% | |||||||||||||||||
Phenothiazine | ✔ | 98% | |||||||||||||||||
Pimozide |
+
Dopamine D1 receptor, Ki: 6600 nM |
+++
Dopamine D2 receptor, Ki: 3.0 nM |
++++
Dopamine D3 receptor, Ki: 0.83 nM |
98% | |||||||||||||||
Rotundine |
++
D1 receptor, IC50: 166 nM |
+
D2 receptor, IC50: 1.47 μM |
+
D3 receptor, IC50: 3.25 μM |
98% | |||||||||||||||
Domperidone | ✔ | 99+% | |||||||||||||||||
ONC206 | ✔ | 99% | |||||||||||||||||
Pimethixene maleate |
++
Dopamine D1 Receptor, pKi: 6.37 |
+++
Dopamine D2 Receptor, pKi: 8.19 |
++
Dopamine D4.4 Receptor, pKi: 7.54 |
97% | |||||||||||||||
Loxapine succinate |
++
D2 receptor (Human), Ki: 62 nM D1 receptor (human), Ki: 26 nM |
++
D2 receptor (human), Ki: 24 nM D2 receptor (bovine), Ki: 26 nM |
+++
D4 receptor (human), Ki: 7.5 nM |
99% | |||||||||||||||
Chlorprothixene |
+++
D1 receptor, Ki: 18 nM |
+++
D2 receptor, Ki: 2.96 nM |
+++
D3 receptor, Ki: 4.56 nM |
+++
D5 receptor, Ki: 9 nM |
99% | ||||||||||||||
SCH-23390 HCl |
++++
D1 dopamine receptor, Ki: 0.2 nM |
++++
D5 dopamine receptor, Ki: 0.3 nM |
98% | ||||||||||||||||
MPP+ iodide | ✔ | 97% | |||||||||||||||||
σ1 Receptor antagonist-1 |
+
DAT, pKi: 5.8 |
97% | |||||||||||||||||
Benztropine mesylate |
++
DAT, IC50: 118 nM |
98% | |||||||||||||||||
Azaperone | ✔ | 98% | |||||||||||||||||
Ziprasidone HCl | ✔ | 98+% | |||||||||||||||||
Paliperidone | ✔ | 98% | |||||||||||||||||
Alizapride HCl | ✔ | 99+% | |||||||||||||||||
Amisulpride | ✔ | 98% | |||||||||||||||||
Quetiapine hemifumarate | ✔ | Adrenergic Receptor | 98% | ||||||||||||||||
Clozapine N-oxide | ✔ | 99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
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 << |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 440-17-5 |
分子式 | C21H26Cl2F3N3S |
分子量 | 480.418 |
别名 | 盐酸三氟拉嗪;三氟吡拉嗪;甲哌氟丙嗪;三氟拉嗪二盐酸盐 ;Trifluoperazine (hydrochloride);SKF5019;Trazine;Tryptazine dihydrochloride;Trifluoperazine HCl;NSC 17474;Trifluoperazine hydrochloride;TFP;Trifluoperazine 2HCl |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Store in freezer, under -20°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 |
PO 0.5% CMC-Na 15 mg/mL suspension |