PD 168077 maleate

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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 (7)
Reviews
Literature (4)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.05 100
ethanol 11.26 25

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References

References are publications that support the biological activity of the product.

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

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

Gu et al (2006) Activation of DA 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: PD 168077 maleate, PD 168077 maleate supplier, High, affinity, selective, D4, agonists, Dopamine, Receptors, dopaminergic, PD168077, maleate, 1065, Tocris Bioscience

7 Citations for PD 168077 maleate

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

Dai et al (2017) Is DA transporter-mediated DArgic signaling in the retina a noninvasive biomarker for attention-deficit/ hyperactivity disorder? A study in a novel DA transporter variant Val559 transgenic mouse model. J Neurodev Disord 9 38 PMID: 29281965

Negrete-Díaz et al (2019) Pharmacological activation of dopamine D4 receptor modulates morphine-induced changes in the expression of GAD65/67 and GABAB receptors in the basal ganglia. Neuropharmacology 152 22 PMID: 30682345

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

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

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

Guo (2017) DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell 16 1323 PMID: 28975698

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


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