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PD 168077 maleate
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.
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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:
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
Graziane et al (2009) DA D4 Receptors Regulate GABAA Receptor Trafficking via an Actin/Cofilin/Myosin-dependent Mechanism. Circ Res 284 8329 PMID: 19179335
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
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
Yuen et al (2013) Restoration of glutamatergic transmission by DA D4 receptors in stressed animals. J Biol Chem 288 26112 PMID: 23884421
Guo (2017) DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell 16 1323 PMID: 28975698
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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.