PD 168077 maleate

Pricing Availability Delivery Time Qty
Cat.No. 1065 - PD 168077 maleate | C20H22N4O.C4H4O4 | CAS No. 630117-19-0
Description: High affinity, selective D4 agonist
Chemical Name: N-(Methyl-4-(2-cyanophenyl)piperazinyl-3-methylbenzamide maleate
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Literature

Biological Activity

A potent D4 dopamine receptor agonist (Ki = 8.7 nM) with > 400-fold selectivity over D2 and > 300-fold selectivity versus D3 subtypes respectively. Induces synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons. Centrally active in vivo.

Technical Data

M. Wt 450.49
Formula C20H22N4O.C4H4O4
Storage Desiccate at -20°C
Purity ≥99% (HPLC)
CAS Number 630117-19-0
PubChem ID 11957665
InChI Key NAEUGRPISCANHO-BTJKTKAUSA-N
Smiles OC(=O)\C=C/C(O)=O.CC1=CC(=CC=C1)C(=O)NCN1CCN(CC1)C1=C(C=CC=C1)C#N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.05 100

Preparing Stock Solutions

The following data is based on the product molecular weight 450.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.22 mL 11.1 mL 22.2 mL
5 mM 0.44 mL 2.22 mL 4.44 mL
10 mM 0.22 mL 1.11 mL 2.22 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Clifford and Waddington (2000) Topographically based search for an "Ethogram" among a series of novel D4 dopamine receptor agonists and antagonists. Neuropsychopharmacology 22 538 PMID: 10731629

Glase et al (1997) Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective dopamine D4 agonists. J.Med.Chem. 40 1771 PMID: 9191952

Gu et al (2006) Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol.Pharmacol. 69 813 PMID: 16365279


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Keywords: High affinity selective D4 agonists Dopamine Receptors dopaminergic PD168077 maleate D4 Receptors

4 Citations for PD 168077 maleate

Citations are publications that use Tocris products. Selected citations for PD 168077 maleate include:

Huang (2017) Neurochemical arguments for the use of dopamine D4 receptor stimulation to improve cognitive impairment associated with schizophrenia. Pharmacol Biochem Behav 157 16 PMID: 28455126

Chen et al (2015) Activation of D4 dopamine receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells. J Biol Chem 65 153 PMID: 25368031

Yuen et al (2013) Restoration of glutamatergic transmission by dopamine D4 receptors in stressed animals. J Biol Chem 288 26112 PMID: 23884421

Graziane et al (2009) Dopamine D4 Receptors Regulate GABAA Receptor Trafficking via an Actin/Cofilin/Myosin-dependent Mechanism. Circ Res 284 8329 PMID: 19179335


Do you know of a great paper that uses PD 168077 maleate from Tocris? If so please let us know.

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