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.
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。
- CAS 番号: 67165-56-4
- 分子式: C17H17Cl2NO
- 分子量:322.23
-
保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-12242
GBR 12935 dihydrochloride -
HY-13217
Vanoxerine dihydrochloride -
HY-13217A
Vanoxerine -
HY-18332C
DOV-216,303 Free Base -
HY-12850A
Dasotraline hydrochloride -
HY-12242R
GBR 12935 dihydrochloride (Standard) -
HY-B1124
Fipexide -
HY-18332A
Amitifadine hydrochloride -
HY-12242A
GBR 12935 -
HY-111928
5,7-Dimethoxyluteolin -
HY-13779
(E/Z)-J147 -
HY-13217R
Vanoxerine dihydrochloride (Standard)
生物活性
製品説明
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Wistar rats (male, 200-250 g)[3]
-
Dosage:10 mg/kg; 20 mg/kg; 50 mg/kg
-
Administration:p.o.; single dose
-
Result:Reduced serum prolactin levels.
化学情報
-
CAS 番号 67165-56-4
-
性状 Liquid (Density: 1.242±0.06 g/cm3)
-
分子量 322.23
-
分子式 C17H17Cl2NO
-
Color Colorless to light yellow
-
SMILES
CN1CC2=C(C=CC(OC)=C2)C(C3=CC=C(Cl)C(Cl)=C3)C1
-
別名
Ro 8-4650
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
純度とドキュメンテーション
-
データシート (277 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-18610A 関連分類
Powered by Bioz