1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. Eticlopride

Eticlopride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride is an antipsychotic agent.

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Eticlopride Chemical Structure

Eticlopride Chemical Structure

CAS No. : 84226-12-0

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Description

Eticlopride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride is an antipsychotic agent[1].

Cellular Effect
Cell Line Type Value Description References
HEK-293T IC50
> 10000 nM
Compound: Eticlopride
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
[PMID: 27933960]
In Vitro

Eticlopride (1 μM, 6 h) abrogates the action of DA, where DA increases KLF2 expression in HUVEC cells[2].
Eticlopride (1 μM, 15 min) abolishes heterodimerization of D2R/SSTR2 in rat striatal neurons[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eticlopride (10 mg/kg, i.p.) blocks normal vessel morphologyc restored by DA in orthotopic PC3 and HT29 tumor-bearing animals[2].
Eticlopride (0.01 or 0.02 mg/kg, i.p.) alleviates cognitive deficits produced by Quinpirole (HY-B1752) in rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats treated with Ruinpirole (1 mg/kg) from postnatal days 1 to 21[4]
Dosage: 0.01 or 0.02 mg/kg
Administration: i.p.
Result: Alleviated cognitive deficits produced by neonatal quinpirole treatment in both male and female rats on the place version of the MWT, as well as in males tested on the match-to-place version of the MwT (MwT tested on P22 to P28).
Molecular Weight

340.85

Formula

C17H25ClN2O3

CAS No.
SMILES

O=C(C1=C(C(CC)=CC(Cl)=C1OC)O)NC[C@H]2N(CCC2)CC

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Purity & Documentation
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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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Eticlopride
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HY-121129
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