PD 168077 maleate

Name: PD 168077 maleate
Brand: tocris
SKU: 1065

Catalog # 1065

Citations (7)

Datasheet / COA / SDS

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Key Product Details

Description:	High affinity, selective D₄ agonist
Chemical Name:	N-(Methyl-4-(2-cyanophenyl)piperazinyl-3-methylbenzamide maleate
Purity:	≥99% (HPLC)
Molecular Weight:	450.49

View Full Technical Details for PD 168077 maleate

Biological Activity

A potent D₄ dopamine receptor agonist (K_i = 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

	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	11.10 mL	22.20 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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References

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

Clifford and Waddington Topographically based search for an "Ethogram" among a series of novel D₄ DA receptor agonists and antagonists. Neuropsychopharmacology 2000 PMID: 10731629
Glase Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective DA D₄ agonists. J.Med.Chem. 1997 PMID: 9191952
Gu Activation of DA D₄ receptors induces synaptic translocation of Ca²⁺/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol.Pharmacol. 2006 PMID: 16365279

Citations (7)

Showing 1 - 7 of 7 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for PD 168077 maleate include:

Negrete-Díaz et al. (2019) Pharmacological activation of dopamine D₄ receptor modulates morphine-induced changes in the expression of GAD_65/67 and GABA_B receptors in the basal ganglia. Neuropharmacology. 152:22
PMID: 30682345
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(6):1323
PMID: 28975698
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
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
Yuen et al. (2013) Restoration of glutamatergic transmission by DA D4 receptors in stressed animals. J Biol Chem. 288:26112
PMID: 23884421
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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Showing 1 - 7 of 7 citations Showing All

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PD 168077 maleate

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Citations (7)

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