PD 168077 maleate

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PD 168077 maleate | CAS No. 630117-19-0 | Dopamine D4 Receptor Agonists
1 Image
Description: High affinity, selective D4 agonist

Chemical Name: N-[[4-(2-Cyanophenyl)-1-piperazinyl]methyl]-3-methylbenzamide maleate

Purity: ≥98%

Product Details
Citations (7)
Reviews

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

M.Wt:
450.49
Formula:
C20H22N4O.C4H4O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
630117-19-0

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

  1. 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.
  2. 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.
  3. 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.
  4. Topographically based search for an "Ethogram" among a series of novel D4 DA receptor agonists and antagonists.
    Clifford and Waddington
    Neuropsychopharmacology, 2000;22:538
  5. 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
  6. Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective DA D4 agonists.
    Glase et al.
    J.Med.Chem., 1997;40:1771

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