1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. PD-168077

PD-168077 is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

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PD-168077

PD-168077 Chemische Struktur

CAS. Nr. : 190383-31-4

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Beschreibung

PD-168077 is a selective dopamine D4 receptor agonist, with a Ki of 9 nM[1].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
17 nM
Compound: 6
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
[PMID: 9191952]
HEK293 EC50
8.3 nM
Compound: 2
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
HEK293 EC50
8.3 nM
Compound: 2, PD-168077
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
> 10 μM
Compound: 2
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
HEK293 IC50
> 10 μM
Compound: 2
Antagonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
Antagonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
In Vitro

In the PD-168077-treated cell, p-CaMKII exhibits a significantly increased clustering at synaptic sites, as indicated by the enhanced colocalization with PSD-95[2].

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

In Vivo

PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced[1].

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

Molekulargewicht

334.41

Formel

C20H22N4O

CAS. Nr.
SMILES

O=C(NCN1CCN(C2=CC=CC=C2C#N)CC1)C3=CC=CC(C)=C3

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Reinheit & Dokumentation
Verweise
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  • Molaritätsrechner

  • Verdünnungsrechner

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Mass   Concentration   Volume   Molecular Weight *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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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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PD-168077
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