Opipramol
Based on 1 Customer Validation
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).
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- Purity: 99.91%
- CAS No.: 315-72-0
- 화학식: C23H29N3O
- 분자량:363.50
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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All Sigma Receptor Isoforms
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Biological Activity
Ki: 50 nM (σ receptor); IC50: 5.5 μM ([3H] DA)[1].
Opipramol can potently interact with sigma recognition sites with a Ki value of 50 nM[1].
Opipramol inhibit the uptake of [3H] DA in crude synaptosomal preparations with an IC50 value of 5.5 μM[1].
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:Sprague-Dawley rats (male, 150-l 80 g)[2]
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Dosage:5-50 mg/kg
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Administration:Intraperitoneal injections
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Result:Increased the levels of DOPAC and HVA in the striatum of the rat, without changing the steady-state levels of DA.
Potently increased the metabolism of dopamine in the striatum, olfactory tubercle and pyriform cortex of the rat.
Increased plasma prolactin in the rat, only at a dose as large as 50 mg/kg dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 315-72-0
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Appearance Solid
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분자량 363.50
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화학식 C23H29N3O
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Color Light yellow to yellow
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SMILES
OCCN1CCN(CCCN2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1
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Synonyms
Ensidon; G-33040
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (275.10 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. H J Möller, et al. Opipramol for the treatment of generalized anxiety disorder: a placebo-controlled trial including an alprazolam-treated group. J Clin Psychopharmacol. 2001 Feb;21(1):59-65. [Content Brief]
[2]. T S Rao, et al. Neurochemical characterization of dopaminergic effects of opipramol, a potent sigma receptor ligand, in vivo. Neuropharmacology. 1990 Dec;29(12):1191-7. [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. 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 | 2.7510 mL | 13.7552 mL | 27.5103 mL | 68.7758 mL |
| 5 mM | 0.5502 mL | 2.7510 mL | 5.5021 mL | 13.7552 mL | |
| 10 mM | 0.2751 mL | 1.3755 mL | 2.7510 mL | 6.8776 mL | |
| 15 mM | 0.1834 mL | 0.9170 mL | 1.8340 mL | 4.5851 mL | |
| 20 mM | 0.1376 mL | 0.6878 mL | 1.3755 mL | 3.4388 mL | |
| 25 mM | 0.1100 mL | 0.5502 mL | 1.1004 mL | 2.7510 mL | |
| 30 mM | 0.0917 mL | 0.4585 mL | 0.9170 mL | 2.2925 mL | |
| 40 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7194 mL | |
| 50 mM | 0.0550 mL | 0.2751 mL | 0.5502 mL | 1.3755 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4585 mL | 1.1463 mL | |
| 80 mM | 0.0344 mL | 0.1719 mL | 0.3439 mL | 0.8597 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6878 mL |
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