PD 168077 maleate
Chemical Name: N-[[4-(2-Cyanophenyl)-1-piperazinyl]methyl]-3-methylbenzamide maleate
Purity: ≥98%
Biological Activity
PD 168077 maleate is 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
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.
Background References
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Endophilin marks and controls a clathrin-independent endocytic pathway.
Boucrot E, Ferreira A, Almeida-Souza L, Debard S, Vallis Y, Howard G, Bertot L, Sauvonnet N, McMahon H
Nature, 2015;517(7535):460-5. -
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Dopamine inhibits the effector functions of activated NK cells via the upregulation of the D5 receptor.
Mikulak J, Bozzo L, Roberto A, Pontarini E, Tentorio P, Hudspeth K, Lugli E, Mavilio D
J Immunol, 2014;193(6):2792-800. -
Topographically based search for an "Ethogram" among a series of novel D4 DA receptor agonists and antagonists.
Clifford and Waddington
Neuropsychopharmacology, 2000;22:538 -
Activation of DA D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons.
Gu et al.
Mol.Pharmacol., 2006;69:813 -
Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective DA D4 agonists.
Glase et al.
J.Med.Chem., 1997;40:1771
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Citations for PD 168077 maleate
The citations listed below are publications that use Tocris products. Selected citations for PD 168077 maleate include:
7 Citations: Showing 1 - 7
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Pharmacological activation of dopamine D4 receptor modulates morphine-induced changes in the expression of GAD65/67 and GABAB receptors in the basal ganglia.
Authors: Negrete-Díaz Et al.
Neuropharmacology 2019;152:22
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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.
Authors: Dai Et al.
J Neurodev Disord 2017;9:38
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DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice.
Authors: Guo
Aging Cell 2017;16(6):1323
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Neurochemical arguments for the use of DA D4 receptor stimulation to improve cognitive impairment associated with schizophrenia.
Authors: Huang
Pharmacol Biochem Behav 2017;157:16
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Activation of D4 DA receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells.
Authors: Chen Et al.
J Biol Chem 2015;65:153
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Restoration of glutamatergic transmission by DA D4 receptors in stressed animals.
Authors: Yuen Et al.
J Biol Chem 2013;288:26112
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DA D4 Receptors Regulate GABAA Receptor Trafficking via an Actin/Cofilin/Myosin-dependent Mechanism.
Authors: Graziane Et al.
Circ Res 2009;284:8329
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