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Sertindole/舍吲哚 {[allProObj[0].p_purity_real_show]}

货号:A495787 同义名: Lu 23-174

Sertindole是一种神经安定剂,是一种抗精神病药,具有较高的亲和力,能与多巴胺 D2、血清素 5-HT2A、5-HT2C 和 α1-肾上腺素受体结合。

Sertindole/舍吲哚 化学结构 CAS号:106516-24-9
Sertindole/舍吲哚 化学结构
CAS号:106516-24-9
Sertindole/舍吲哚 3D分子结构
CAS号:106516-24-9
Sertindole/舍吲哚 化学结构 CAS号:106516-24-9
Sertindole/舍吲哚 3D分子结构 CAS号:106516-24-9
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Sertindole/舍吲哚 纯度/质量文件 产品仅供科研

货号:A495787 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 98% (HPLC)
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole HCl ++

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

98%
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。

Sertindole/舍吲哚 生物活性

描述 Sertindole, a neuroleptic, is one of the antipsychotic medications available. Sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors[3]. Sertindole is at least as effective as haloperidol and risperidone against the positive symptoms of schizophrenia, while it appears superior against negative symptoms. Sertindole is associated with a low rate of extrapyramidal side effects, lacks sedative properties, and may induce a moderate weight gain[4]. The incidence of QTc interval prolongation of 500 ms or greater with therapeutic dosages of sertindole has also been low. Unlike other antipsychotic agents, sertindole has not been associated with cognitive impairment, and can actually improve cognitive function[5]. Long-term treatment with sertindole was safe and well tolerated, and patients showed clinical improvement beyond acute treatment[6].

Sertindole/舍吲哚 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
NCT02374567 Dementia Depr... 展开 >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders 收起 << Phase 3 Terminated - Germany ... 展开 >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany 收起 <<
NCT02307396 Schizophrenia ... 展开 >> Schizophrenia and Disorders With Psychotic Features Schizoaffective Disorders 收起 << Phase 4 Completed - Germany ... 展开 >> Psychiatrische Klinik und Poliklinik fuer Psychiatrie und Psychotherapie der Technischen Universitaet Muenchen am Klinikum rechts der Isar Munich, Bavaria, Germany, 81675 收起 <<
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 <<

Sertindole/舍吲哚 参考文献

[1]Juruena MF, de Sena EP, et al. Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis. 2011 May 17;3:75-85.

[2]Murdoch D, Keating GM. Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55.

[3]Juruena MF, de Sena EP, de Oliveira IR. Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis. 2011 May 17;3:75-85

[4]Spina E, Zoccali R. Sertindole: pharmacological and clinical profile and role in the treatment of schizophrenia. Expert Opin Drug Metab Toxicol. 2008 May;4(5):629-38

[5]Perquin L, Steinert T. A review of the efficacy, tolerability and safety of sertindole in clinical trials. CNS Drugs. 2004;18 Suppl 2:19-30; discussion 41-3

[6]Hale AS, Azorin JM, Lemming OM, Mæhlum E. Sertindole in the long-term treatment of schizophrenia. Int Clin Psychopharmacol. 2012 Jul;27(4):231-7

Sertindole/舍吲哚 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.34mL

2.27mL

1.13mL

22.68mL

4.54mL

2.27mL

Sertindole/舍吲哚 技术信息

CAS号106516-24-9
分子式C24H26ClFN4O
分子量 440.94
SMILES Code FC1=CC=C(N2C3=CC=C(Cl)C=C3C(C4CCN(CCN5CCNC5=O)CC4)=C2)C=C1
MDL No. MFCD00867749
别名 Lu 23-174
运输蓝冰
InChI Key GZKLJWGUPQBVJQ-UHFFFAOYSA-N
Pubchem ID 60149
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 25 mg/mL(56.7 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

请根据您的动物给药指南选择适当的溶解方案。
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
方案一
方案二
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