Ecopipam hydrobromide
Based on 1 Customer Validation
Ecopipam (SCH 39166) hydrobromide 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 hydrobromide 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 hydrobromide can be used for the research of schizophrenia and obesity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.0%
- CAS. Nr.: 2587360-22-1
- Formel: C19H21BrClNO
- Molecular Weight:394.73
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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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 |
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| HepG2 | EC50 |
12.6 μM
Compound: Ecopipam
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
4 μM
Compound: Ecopipam
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
Ecopipam (2 μM) hydrobromide 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 (5 and 10 μM, perfusion, 1 μL/min) 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 were 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2587360-22-1
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Appearance Solid
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Molecular Weight 394.73
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Formel C19H21BrClNO
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Color White to off-white
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SMILES
CN1[C@]2([H])[C@@](C3=CC=CC=C3CC2)([H])C4=CC(O)=C(Cl)C=C4CC1.Br
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Synonyms
SCH 39166 hydrobromide
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Ecopipam hydrobromide Related Classifications
HY-110033 Related Classifications
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