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PD-168077

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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

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

CAS No.: 190383-31-4
Formula: C₂₀H₂₂N₄O
Molecular Weight:334.41

Storage:

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

Data Sheet (270 KB)

PD-168077 Chemical Structure

CAS No.: 190383-31-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

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

All Dopamine Receptor Isoforms :

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	>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	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	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.

Chemical Information

CAS No. 190383-31-4
Molecular Weight 334.41
Formula C₂₀H₂₂N₄O
SMILES

O=C(NCN1CCN(C2=CC=CC=C2C#N)CC1)C3=CC=CC(C)=C3
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Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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Research Square Preprint

2023 Oct 3.

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Clifford JJ, et al. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology. 2000 May;22(5):538-44. [Content Brief]

[2]. Gu Z, et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol Pharmacol. 2006 Mar;69(3):813-22. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References

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PD-168077

Publications Citing Use of MedChemExpress (MCE) PD-168077

All Dopamine Receptor Isoforms