Fluphenazine decanoate 是一种多巴胺D2受体抑制剂和吩噻嗪类精神安定剂 (neuroleptic)。Fluphenazine decanoate可用于精神分裂症的研究。
| 生物活性 | Fluphenazine decanoate is adopamineD2receptorinhibitor, is a long-acting phenothiazineneuroleptic. Fluphenazine can be used for schizophrenia research[1][2][3]. |
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体外研究
(In Vitro) | Fluphenazine decanoate shows activity againstT. gondiiin human fibroblast cell cultures with an IC50value of 1.7 mM[1].
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体内研究
(In Vivo) | Fluphenazine decanoate (0.22 mg/kg and followed by 0.33 mg/kg; i.m.; 8 times every 3 weeks), as an antipsychotic, increases sensitivity to dopamine on monkey model following extended treatment[2].
Fluphenazine decanoate (25 mg/kg; i.m.; 6 times every 3 weeks; 24 weeks) induces mouth movements in the rat, serves as a pharmacological model of human tardive dyskinesia[3].
Fluphenazine decanoate (1, 2, 3 mg/kg/d; s.c.; 60 d) shows antifertility effects and induces hyperprolactinemia concomitant with gonadotropin suppression in adult male rat[4].
| Animal Model: | Cebus apella monkey[2] | | Dosage: | 0.22 mg/kg and followed by 0.33 mg/kg | | Administration: | Intramuscular injection; 8 times per 3 weeks; 0.22 mg/kg for 63 weeks and 0.33 mg/kg for 6 weeks | | Result: | Decreased the aggressiveness composite behavioral variables (CBV).
Resulted stereotypic behavior induced by agonist and decreased prolactin response to AMPH. |
| Animal Model: | Male Sprague-Dawley rats (250 g)[3] | | Dosage: | 25 mg/kg | | Administration: | Intramuscular injection into the hind limb; 24 weeks | | Result: | Resulted in spontaneous vacuous chewing mouth movements and jaw tremor. |
| Animal Model: | Adult male rats[4] | | Dosage: | 1, 2, 3 mg/kg/d | | Administration: | Subcutaneous injection between 10:00-12:00 h; 60 days | | Result: | Increased serum prolactin level and suppressed serum LH and FSH levels at day 60.
Increased hypothalamic tyrosine hydroxylase levels, enhanced chromatin decondensation, and resulted DNA denaturation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(211.23 mM;Need ultrasonic) Ethanol : 50 mg/mL(84.49 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6898 mL | 8.4492 mL | 16.8985 mL | | 5 mM | 0.3380 mL | 1.6898 mL | 3.3797 mL | | 10 mM | 0.1690 mL | 0.8449 mL | 1.6898 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.08 mg/mL (1.83 mM); Clear solution
此方案可获得 ≥ 1.08 mg/mL (1.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.08 mg/mL (1.83 mM); Clear solution
此方案可获得 ≥ 1.08 mg/mL (1.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.08 mg/mL (1.83 mM); Clear solution
此方案可获得 ≥ 1.08 mg/mL (1.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 10.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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