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+ |
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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。 |
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]. |
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 << | |
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 |
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 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
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