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Ziprasidone HCl monohydrate/佐帕司通 {[allProObj[0].p_purity_real_show]}

货号:A473367 同义名: 盐酸齐拉西酮水合物;齐拉西酮盐酸盐一水合物 / CP-88,059; Ziprasidone (hydrochloride hydrate)

Ziprasidone HCl H2O is a full antagonist of D2 receptors and of 5-HT2A receptors and is a partial agonist of 5-HT1A receptors, of 5-HT2C receptors and 5-HT1D receptors, used as an atypical antipsychoticfor the treatment of schizophrenia as well as acute mania and mixed states associated with bipolar disorder.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Ziprasidone HCl monohydrate/佐帕司通 化学结构 CAS号:138982-67-9
Ziprasidone HCl monohydrate/佐帕司通 化学结构
CAS号:138982-67-9
Ziprasidone HCl monohydrate/佐帕司通 3D分子结构
CAS号:138982-67-9
Ziprasidone HCl monohydrate/佐帕司通 化学结构 CAS号:138982-67-9
Ziprasidone HCl monohydrate/佐帕司通 3D分子结构 CAS号:138982-67-9
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Ziprasidone HCl monohydrate/佐帕司通 纯度/质量文件 产品仅供科研

货号:A473367 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 99%
Fluvoxamine maleate 99%
Iloperidone 99%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

95%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron HCl dihydrate 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

95%
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。
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 ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 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。

Ziprasidone HCl monohydrate/佐帕司通 生物活性

描述 Ziprasidone HCl H2O is a full antagonist of D2 receptors and of 5-HT2A receptors and is a partial agonist of 5-HT1A receptors, of 5-HT2C receptors and 5-HT1D receptors, used as an atypical antipsychoticfor the treatment of schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Ziprasidone HCl has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone HCl is an inhibitor of norepinephrine reuptake[2]. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. The compound is well tolerated in animals at doses producing effective dopamine antagonism in the brain[3]. Ziprasidone exhibits dose proportional, linear changes in exposure and is hepatically metabolized primarily by aldehyde oxidase[4]. Short-term treatment with intramuscular ziprasidone was effective and well tolerated in patients with acute agitation associated with psychosis[5].

Ziprasidone HCl monohydrate/佐帕司通 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
NCT01185743 Schizophrenia ... 展开 >> Diabetes 收起 << Phase 4 Completed - Austria ... 展开 >> Medical University of Vienna Vienna, Austria, 1090 收起 <<
NCT00538629 - Completed - -
NCT01598324 - Terminated(Clinical trial from... 展开 >> which subjects were recruited closed to enrollment) 收起 << - United States, Massachusetts ... 展开 >> McLean Hospital - McLean Imaging Center Belmont, Massachusetts, United States, 02478 收起 <<

Ziprasidone HCl monohydrate/佐帕司通 参考文献

[1]Ravikiran A, Arthanareeswari M, et al. Nonisothermal kinetics analysis of the dehydration of ziprasidone hydrochloride monohydrate by thermogravimetry. Indian J Pharm Sci. 2013 May;75(3):361-4.

[2]Rollema H, Lu Y, Schmidt AW, Sprouse JS, Zorn SH. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000 Aug 1;48(3):229-37

[3]Seeger TF, Seymour PA, Schmidt AW, Zorn SH, Schulz DW, Lebel LA, McLean S, Guanowsky V, Howard HR, Lowe JA 3rd, et al. Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther. 1995 Oct;275(1):101-13

[4]Patel NC, Keck PE Jr. Ziprasidone: efficacy and safety in patients with bipolar disorder. Expert Rev Neurother. 2006 Aug;6(8):1129-38

[5]Gunasekara NS, Spencer CM, Keating GM. Ziprasidone: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2002;62(8):1217-51

Ziprasidone HCl monohydrate/佐帕司通 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.39mL

4.28mL

2.14mL

Ziprasidone HCl monohydrate/佐帕司通 技术信息

CAS号138982-67-9
分子式C21H24Cl2N4O2S
分子量 467.41
SMILES Code O=C1CC2=CC(CCN3CCN(C4=NSC5=C4C=CC=C5)CC3)=C(Cl)C=C2N1.[H]Cl.O
MDL No. MFCD00921885
别名 盐酸齐拉西酮水合物;齐拉西酮盐酸盐一水合物 ;CP-88,059; Ziprasidone (hydrochloride hydrate); CP 88059 hydrochloride monohydrate; Ziprasidone hydrochloride monohydrate
运输蓝冰
InChI Key ZCBZSCBNOOIHFP-UHFFFAOYSA-N
Pubchem ID 60853
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 25 mg/mL(53.49 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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