Diclofensine
Diclofensine (Ro 8-46500) is an orally active neuronal monoamine uptake inhibitor. Diclofensine blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine can be used in the research of moderate to severe depression.
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- CAS No.: 67165-56-4
- 화학식: C17H17Cl2NO
- 분자량:322.23
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보관:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
Diclofensine (0.01-1 μM; 13 min) potently inhibits 3H-DA uptake in synaptosomes isolated from the arcuate nucleus-periventricular nucleus-median eminence of rats[3].
Diclofensine (50 μM; 10 min) does not alter the basal endogenous dopamine release from tuberoinfundibular dopaminergic (TIDA) neurons in rats[3].
Diclofensine (50 μM; 20 min) increases the K+-stimulated release of endogenous dopamine by 3-fold in rat tuberoinfundibular dopaminergic (TIDA) neurons[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 200-250 g)[3]
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Dosage:10 mg/kg; 20 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Reduced serum prolactin levels.
Chemical Information
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CAS No. 67165-56-4
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Appearance Liquid (Density: 1.242±0.06 g/cm3)
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분자량 322.23
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화학식 C17H17Cl2NO
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Color Colorless to light yellow
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SMILES
CN1CC2=C(C=CC(OC)=C2)C(C3=CC=C(Cl)C(Cl)=C3)C1
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Synonyms
Ro 8-4650
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (310.34 mM; Need ultrasonic; 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (296 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gasić S, et al. Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function. Clin Pharmacol Ther. 1986;39(5):582-585. [Content Brief]
[2]. Cherpillod C, et al. A controlled trial with diclofensine, a new psychoactive drug, in the treatment of depression. J Int Med Res. 1981;9(5):324-329. [Content Brief]
[3]. Di Renzo G, et al. Pure uptake blockers of dopamine can reduce prolactin secretion: studies with diclofensine. Life Sci. 1988;42(21):2161-2169. [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 (protect from light). 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 |
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| DMSO | 1 mM | 3.1034 mL | 15.5169 mL | 31.0337 mL | 77.5843 mL |
| 5 mM | 0.6207 mL | 3.1034 mL | 6.2067 mL | 15.5169 mL | |
| 10 mM | 0.3103 mL | 1.5517 mL | 3.1034 mL | 7.7584 mL | |
| 15 mM | 0.2069 mL | 1.0345 mL | 2.0689 mL | 5.1723 mL | |
| 20 mM | 0.1552 mL | 0.7758 mL | 1.5517 mL | 3.8792 mL | |
| 25 mM | 0.1241 mL | 0.6207 mL | 1.2413 mL | 3.1034 mL | |
| 30 mM | 0.1034 mL | 0.5172 mL | 1.0345 mL | 2.5861 mL | |
| 40 mM | 0.0776 mL | 0.3879 mL | 0.7758 mL | 1.9396 mL | |
| 50 mM | 0.0621 mL | 0.3103 mL | 0.6207 mL | 1.5517 mL | |
| 60 mM | 0.0517 mL | 0.2586 mL | 0.5172 mL | 1.2931 mL | |
| 80 mM | 0.0388 mL | 0.1940 mL | 0.3879 mL | 0.9698 mL | |
| 100 mM | 0.0310 mL | 0.1552 mL | 0.3103 mL | 0.7758 mL |
Diclofensine Related Classifications
HY-18610A Related Classifications
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