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Molindone HCl

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Chemical Structure| 15622-65-8 同义名 : 盐酸吗啉吲酮 ;EN-1733A;Molindone (hydrochloride);Moban;Molindone HCl salt;Molindone Hydrochloride salt;(±)-Molindone;Molindone hydrochloride
CAS号 : 15622-65-8
货号 : A653237
分子式 : C16H25ClN2O2
纯度 : 98%
分子量 : 312.835
MDL号 : MFCD01718304
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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:
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].
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 - -
实验方案
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

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