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盐酸吗茚酮 /Molindone HCl {[allProObj[0].p_purity_real_show]}

货号:A653237 同义名: 盐酸吗啉吲酮 / EN-1733A;Molindone (hydrochloride)

Molindone HCl, the salt form of molindone which is a dopamine receptor antagonist, can be used in the treatment of schizophrenia and act as a therapeutic antipsychotic.

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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+
Molindone HCl 化学结构 CAS号:15622-65-8
Molindone HCl 化学结构
CAS号:15622-65-8
Molindone HCl 3D分子结构
CAS号:15622-65-8
Molindone HCl 化学结构 CAS号:15622-65-8
Molindone HCl 3D分子结构 CAS号:15622-65-8
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Molindone HCl 纯度/质量文件 产品仅供科研

货号:A653237 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

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
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 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
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 97%
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

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
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。

Molindone HCl 生物活性

靶点
  • D2 receptor

描述 Molindone hydrochloride, a dihydroindolone neuroleptic, is structurally distinct from other classes of neuroleptics. Molindone exhibits many similarities to other neuroleptics, including dopamine receptor blockade, antipsychotic efficacy, and extrapyramidal side effects. Clinically, molindone has a tendency to cause weight loss and may have less effect on seizure threshold than conventional antipsychotic agents[3]. Molindone is a relatively safe neuroleptic for child and adolescent inpatients because of its short half-life and minimal prolonged tissue accumulation[4]. Molindone at doses of 5-20 mg/day (children weighing <30 kg) and 20-40 mg (≥ 30 kg) was well tolerated, and preliminary efficacy results suggest that molindone produces dose-related behavioral improvements over 9-12 weeks[5]. Once a patient's acute psychotic episode has been stabilized with intramuscular molindone, therapy can continue without interruption by substituting 1.5 mg of oral molindone for every 1 mg of intramuscular molindone. The time to maximum concentration occurred significantly earlier with intramuscular molindone (0.6 hours) than with oral molindone (1.1 hours) [6].

Molindone HCl 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
NCT00053703 Schizophrenia Phase 4 Completed - United States, Massachusetts ... 展开 >> Cambridge Health Alliance Medford, Massachusetts, United States, 02155 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27514 United States, Ohio University Hospitals of Cleveland Cleveland, Ohio, United States, 44106 United States, Washington University of Washington Seattle, Washington, United States, 98195 收起 <<
NCT01416064 Impulsive Aggression Comorbid ... 展开 >>With ADHD in Children 收起 << Phase 2 Completed - -
NCT00053703 - Completed - -

Molindone HCl 参考文献

[1]Krishna G, Gopalakrishnan G, et al. In vitro and in vivo genotoxicity assessment of the dopamine receptor antagonist molindone hydrochloride. Environ Mol Mutagen. 2016 May;57(4):288-98.

[2]Owen RR Jr, Cole JO. Molindone hydrochloride: a review of laboratory and clinical findings. J Clin Psychopharmacol. 1989 Aug;9(4):268-76.

[3]Owen RR Jr, Cole JO. Molindone hydrochloride: a review of laboratory and clinical findings. J Clin Psychopharmacol. 1989;9(4):268‐276

[4]Greenhill LL, Solomon M, Pleak R, Ambrosini P. Molindone hydrochloride treatment of hospitalized children with conduct disorder. J Clin Psychiatry. 1985;46(8 Pt 2):20‐25

[5]Stocks JD, Taneja BK, Baroldi P, Findling RL. A phase 2a randomized, parallel group, dose-ranging study of molindone in children with attention-deficit/hyperactivity disorder and persistent, serious conduct problems. J Child Adolesc Psychopharmacol. 2012;22(2):102‐111

[6]Zetin M, Cramer M, Garber D, et al. Bioavailability of oral and intramuscular molindone hydrochloride in schizophrenic patients. Clin Ther. 1985;7(2):169‐175

Molindone HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

15.98mL

3.20mL

1.60mL

31.97mL

6.39mL

3.20mL

Molindone HCl 技术信息

CAS号15622-65-8
分子式C16H25ClN2O2
分子量 312.835
别名 盐酸吗啉吲酮 ;EN-1733A;Molindone (hydrochloride);Moban;Molindone HCl salt;Molindone Hydrochloride salt;(±)-Molindone;Molindone hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 16 mg/mL(51.15 mM),配合低频超声,并水浴加热至45℃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: 100 mg/mL(319.66 mM),配合低频超声助溶

动物实验配方
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