Ecopipam hydrochloride
Based on 1 Customer Validation
Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 190133-94-9
- Formula: C19H21Cl2NO
- Molecular Weight:350.28
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Dopamine Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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D1 Receptor 1.2 nM (Ki) |
D5 Receptor 2.0 nM (Ki) |
D2 Receptor 980 nM (Ki) |
D4 Receptor 5520 nM (Ki) |
5-HT Receptor 80 nM (Ki) |
Alpha-2A adrenergic receptor 731 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
1.5 nM
Compound: SCH 39166
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Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
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[PMID: 32631525] |
Ecopipam (2 μM) hydrochloride completely abolishes the proconvulsive effect of Dopamine (10 μM) in isolated corticohippocampal formation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ecopipam (10, mg/kg, oral administration) hydrochloride antagonizes Apomorphine-induced stereotypy in rats[4].
Ecopipam (5 and 10 μM, perfusion, 1 μL/min) hydrochloride reversibly and dose-dependently decreases acetylcholine release in the rat striatum[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male young adult Long-Evans rats injected with Nicotine[3]
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Dosage:0.003, 0.01, 0.03, 0.1, 0.3 mg/kg
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Administration:A single s.c. 20 min before Nicotine (0.1 mg/kg)
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Result:Dose-dependently reduced pressing on both active and inactive levers.
Chemical Information
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CAS No. 190133-94-9
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Appearance Solid
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Molecular Weight 350.28
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Formula C19H21Cl2NO
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Color White to off-white
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SMILES
OC1=C(Cl)C=C2C([C@]3([H])[C@@](CCC4=C3C=CC=C4)([H])N(C)CC2)=C1.[H]Cl
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Synonyms
SCH 39166 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (285.49 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 (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.
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.
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 (7.14 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.14 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Wu WL, et, al. Dopamine D1/D5 receptor antagonists with improved pharmacokinetics: design, synthesis, and biological evaluation of phenol bioisosteric analogues of benzazepine D1/D5 antagonists. J Med Chem. 2005 Feb 10;48(3):680-93. [Content Brief]
[2]. Sharopov S, et al. Dopaminergic modulation of low-Mg²⁺-induced epileptiform activity in the intact hippocampus of the newborn mouse in vitro. J Neurosci Res. 2012 Oct;90(10):2020-33. [Content Brief]
[3]. Satanove DJ, et al. Nicotine-induced enhancement of a sensory reinforcer in adult rats: antagonist pretreatment effects. Psychopharmacology (Berl). 2021 Feb;238(2):475-486. [Content Brief]
[4]. R E Chipkin, et al. Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity. J Pharmacol Exp Ther. 1988 Dec;247(3):1093-102. [Content Brief]
[5]. E Acquas, et al. Local application of SCH 39166 reversibly and dose-dependently decreases acetylcholine release in the rat striatum. Eur J Pharmacol. 1999 Nov 3;383(3):275-9. [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 | 1 mM | 2.8549 mL | 14.2743 mL | 28.5486 mL | 71.3715 mL |
| 5 mM | 0.5710 mL | 2.8549 mL | 5.7097 mL | 14.2743 mL | |
| 10 mM | 0.2855 mL | 1.4274 mL | 2.8549 mL | 7.1371 mL | |
| 15 mM | 0.1903 mL | 0.9516 mL | 1.9032 mL | 4.7581 mL | |
| 20 mM | 0.1427 mL | 0.7137 mL | 1.4274 mL | 3.5686 mL | |
| 25 mM | 0.1142 mL | 0.5710 mL | 1.1419 mL | 2.8549 mL | |
| 30 mM | 0.0952 mL | 0.4758 mL | 0.9516 mL | 2.3790 mL | |
| 40 mM | 0.0714 mL | 0.3569 mL | 0.7137 mL | 1.7843 mL | |
| 50 mM | 0.0571 mL | 0.2855 mL | 0.5710 mL | 1.4274 mL | |
| 60 mM | 0.0476 mL | 0.2379 mL | 0.4758 mL | 1.1895 mL | |
| 80 mM | 0.0357 mL | 0.1784 mL | 0.3569 mL | 0.8921 mL | |
| 100 mM | 0.0285 mL | 0.1427 mL | 0.2855 mL | 0.7137 mL |
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