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

PD-168077 maleate 

Cat. No.: HY-21098A Purity: 98.44%
Handling Instructions

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

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

PD-168077 maleate Chemical Structure

PD-168077 maleate Chemical Structure

CAS No. : 630117-19-0

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10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 150 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

Ki: 9 nM (Dopamine D4 receptor)[1].

In Vitro

PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It shows >100-fold selectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077 shows a 20-fold selectivity over α1, and α2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over 5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 receptor in terms of quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake in CHO cells expressing the human D4 receptor[1]. 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].

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].

Molecular Weight

450.49

Formula

C₂₄H₂₆N₄O₅

CAS No.

630117-19-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (332.97 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2198 mL 11.0990 mL 22.1981 mL
5 mM 0.4440 mL 2.2198 mL 4.4396 mL
10 mM 0.2220 mL 1.1099 mL 2.2198 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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PD-168077 maleate
Cat. No.:
HY-21098A
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