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

Ecopipam (SCH 39166) 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 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 can be used for the research of schizophrenia and obesity.

For research use only. We do not sell to patients.

Ecopipam Chemical Structure

Ecopipam Chemical Structure

CAS No. : 112108-01-7

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Description

Ecopipam (SCH 39166) 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 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 can be used for the research of schizophrenia and obesity[1][3].

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)

In Vitro

Ecopipam (2 μM) 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 (0.003-0.3 mg/kg; a single s.c.) abolishes Nicotine-induced enhancement of a sensory reinforcer in adult rats[3].
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 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.
Clinical Trial
Molecular Weight

313.82

Formula

C19H20ClNO

CAS No.
SMILES

OC1=C(Cl)C=C2C([C@]3([H])[C@@](CCC4=C3C=CC=C4)([H])N(C)CC2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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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Ecopipam
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HY-14690
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