Molindone (hydrochloride)
Based on 1 Customer Validation
Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.81%
- CAS 番号: 15622-65-8
- 分子式: C16H25ClN2O2
- 分子量:312.83
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Dopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
D2 Receptor |
D5 Receptor |
体外実験
Molindone hydrochloride scarcely affects rat brain MAO activity in vitro, with a IC50 of 9.8 × 10-3 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Molindone hydrochloride (5-75 mg/kg-bw/day; i.g.; daily; 8 weeks) induces dose-dependent CNS effects, body weight and food consumption reductions in males, serum chemistry alterations, organ weight changes, and delays in sexual maturation (attributed to reduced body weights), with most effects resolving during a 6-week non-dosing recovery period; no significant adverse effects on reproductive function are observed when administered orally to juvenile CD Sprague-Dawley rats[1].
Molindone hydrochloride (p.o.) exhibits neuroleptic and antidepressant activityin rats[2].
Molindone hydrochloride (1-2 mg/kg; p.o.) blocks Apomorphine (HY-12723)-induced emesis in dogs[2].
Molindone hydrochloride (0.5-1 mg/kg; p.o.) reduces aggressiveness for 2-3 hours, with higher doses producing gradual, sustained docility in Macaca mulatta[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GF1 mice (male)[2]
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Dosage:2.5 mg/kg (tetrabenazine-induced ptosis ED50); 10.0 mg/kg (5-HTP potentiation ED50); 12.0 mg/kg (DOPA potentiation ED50); 5-15 mg/kg (catalepsy, hypothermia)
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Administration:p.o.; 1 hour before test assessment
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Result:Suppressed spontaneous locomotion, blocked conditioned avoidance responses, and antagonized amphetamine-induced stereotyped behaviour; relative potency vs.
chlorpromazine was 0.23 (locomotor suppression), 0.17 (avoidance blockade), and 0.31 (amphetamine antagonism).
Achieved an ED50 of 2.5 mg/kg for antagonizing tetrabenazine-induced ptosis.
Achieved an ED50 of 10.0 mg/kg for potentiating 5-hydroxytryptophan (5-HTP) effects.
Achieved an ED50 of 12.0 mg/kg for potentiating 3,4-dihydroxyphenylalanine (DOPA) effects.
Induced catalepsy and hypothermia at oral doses of 5-15 mg/kg.
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Animal Model:Rhesus monkey[2]
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Dosage:0.5, 1 mg/kg
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Administration:p.o.
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Result:Curtailed aggressiveness for 2-3 hours at oral doses of 0.5-1 mg/kg.
Increasing doses gradually increased the degree and duration of docility, with a more gradual response than chlorpromazine.
化学情報
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CAS 番号 15622-65-8
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性状 Solid
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分子量 312.83
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分子式 C16H25ClN2O2
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Color White to off-white
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SMILES
O=C1C2=C(NC(C)=C2CC)CCC1CN3CCOCC3.[H]Cl
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別名
モリンドン塩酸塩; EN-1733A
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
H2O : 100 mg/mL (319.66 mM; Need ultrasonic)
DMSO : 17.5 mg/mL (55.94 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (480 KB)
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- Portuguese - PT (480 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Krishna G, et al. Toxicity assessment of molindone hydrochloride, a dopamine D2/D5 receptor antagonist in juvenile and adult rats. Toxicol Mech Methods. 2017;27(5):352-362. [Content Brief]
[2]. Rubin A A, et al. Psychopharmacological profile of molindone[J]. Nature, 1967, 216(5115): 578-579. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.1966 mL | 15.9831 mL | 31.9662 mL | 79.9156 mL |
| 5 mM | 0.6393 mL | 3.1966 mL | 6.3932 mL | 15.9831 mL | |
| 10 mM | 0.3197 mL | 1.5983 mL | 3.1966 mL | 7.9916 mL | |
| 15 mM | 0.2131 mL | 1.0655 mL | 2.1311 mL | 5.3277 mL | |
| 20 mM | 0.1598 mL | 0.7992 mL | 1.5983 mL | 3.9958 mL | |
| 25 mM | 0.1279 mL | 0.6393 mL | 1.2786 mL | 3.1966 mL | |
| 30 mM | 0.1066 mL | 0.5328 mL | 1.0655 mL | 2.6639 mL | |
| 40 mM | 0.0799 mL | 0.3996 mL | 0.7992 mL | 1.9979 mL | |
| 50 mM | 0.0639 mL | 0.3197 mL | 0.6393 mL | 1.5983 mL | |
| H2O | 60 mM | 0.0533 mL | 0.2664 mL | 0.5328 mL | 1.3319 mL |
| 80 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9989 mL | |
| 100 mM | 0.0320 mL | 0.1598 mL | 0.3197 mL | 0.7992 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Molindone (hydrochloride) 関連分類
HY-B1017 関連分類
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