1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor 5-HT Receptor Adrenergic Receptor
  3. Ecopipam hydrobromide

Ecopipam hydrobromide  (Synonyms: SCH 39166 hydrobromide)

Cat. No.: HY-110033 Pureza: 99.0%
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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.

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Ecopipam hydrobromide

Ecopipam hydrobromide Estructura química

No. CAS : 2587360-22-1

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Descripciòn

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[1].

IC50 & Target[1]

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)

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
12.6 μM
Compound: Ecopipam
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
[PMID: 20966043]
HepG2 EC50
4 μM
Compound: Ecopipam
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
[PMID: 20966043]
In Vitro

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.

In Vivo

Ecopipam (10, mg/kg, oral administration) antagonizes Apomorphine-induced stereotypy in rats[4].
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.

Animal Model: Male young adult Long-Evans rats were injected with Nicotine[3]
Dosage: 0.003, 0.01, 0.03, 0.1, 0.3 mg/kg
Administration: A single s.c. 20 min before Nicotine (0.1 mg/kg)
Result: Dose-dependently reduced pressing on both active and inactive levers.
Ensayo clínico
Peso molecular

394.73

Fòrmula

C19H21BrClNO

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

CN1[C@]2([H])[C@@](C3=CC=CC=C3CC2)([H])C4=CC(O)=C(Cl)C=C4CC1.Br

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Ecopipam hydrobromide
Cat. No.:
HY-110033
Cantidad:
MCE Japan Authorized Agent: