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

Eticlopride, a potent and selective D2 receptor antagonist, was investigated in rats with extensive dopamine denervation induced by 6-hydroxydopamine. Daily injections of eticlopride over 21 days increased D2 receptor density in intact brain regions but did not further augment already increased densities in denervated areas. Despite receptor density changes, functional sensitivity remained evident, as shown by contralateral rotations induced by D2 agonist quinpirole during wash-out periods. The study suggests that chronic D2 receptor blockade and dopamine denervation may share a common mechanism in upregulating D2 receptor density, contrary to previous reports suggesting additive effects of denervation and antagonist treatment.

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Eticlopride Chemical Structure

Eticlopride Chemical Structure

CAS No. : 84226-12-0

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Description

Eticlopride, a potent and selective D2 receptor antagonist, was investigated in rats with extensive dopamine denervation induced by 6-hydroxydopamine. Daily injections of eticlopride over 21 days increased D2 receptor density in intact brain regions but did not further augment already increased densities in denervated areas. Despite receptor density changes, functional sensitivity remained evident, as shown by contralateral rotations induced by D2 agonist quinpirole during wash-out periods. The study suggests that chronic D2 receptor blockade and dopamine denervation may share a common mechanism in upregulating D2 receptor density, contrary to previous reports suggesting additive effects of denervation and antagonist treatment[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]
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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Eticlopride
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