A dopamine D4 receptor agonist
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PD 168077 (maleate)

Item No. 29789

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[4-(2-cyanophenyl)-1-piperazinyl]methyl]-3-methyl-benzamide, (2Z)-2-butenedioate
CAS Number
630117-19-0
Molecular Formula
C20H22N4O • C4H4O4
Formula Weight
450.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/mlEthanol: insolubl
λmax
220 nm
SMILES
CC1=CC=CC(C(NCN2CCN(C3=C(C#N)C=CC=C3)CC2)=O)=C1.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C20H22N4O.C4H4O4/c1-16-5-4-7-17(13-16)20(25)22-15-23-9-11-24(12-10-23)19-8-3-2-6-18(19)14-21;5-3(6)1-2-4(7)8/h2-8,13H,9-12,15H2,1H3,(H,22,25);1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
NAEUGRPISCANHO-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $183

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    25 mg

    $402

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    50 mg

    $702

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    Product Description

    PD 168077 is a dopamine D4 receptor agonist (Ki = 8.7 nM in CHO Pro 5 cells expressing the human receptor).1 It is selective for dopamine D4 over D2 and D3 receptors (Kis = 3,740 and 2,810 nM, respectively), as well as α1- and α2-adrenergic and serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2A (Kis = 168, 177, 385, and 4,010 nM, respectively). PD 168077 (20 µM) induces CaMKII translocation from the dendritic shaft to postsynaptic sites on the dendritic processes of primary rat embryonic prefrontal cortex pyramidal neurons, an effect that can be blocked by the IP3 receptor antagonist 2APB or the calcium chelator BAPTA AM (Item No. 15551).2 PD 168077 (50-200 ng/animal) induces penile erections in rats when injected into the paraventricular nucleus (PVN) of the hypothalamus.3 PD 168077 (0.2-25 mg/kg, s.c.) increases spontaneous locomotor activity and reduces grooming and rearing in rats.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Glase, S.A., Akunne, H.C., Georgic, L.M., et al. Substituted [(4-phenylpiperazinyl)-methyl]benzamides: Selective dopamine D4 agonists. J. Med. Chem. 40(12), 1771-1772 (1997).

    2. Gu, Z., Jiang, Q., Yuen, E.Y., et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol. Pharmacol. 69(3), 813-822 (2005).

    3. Melis, M.R., Succu, S., Mascia, M.S., et al. PD-168077, a selective dopamine D4 receptor agonist, induces penile erection when injected into the paraventricular nucleus of male rats. Neurosci. Lett. 379(1), 59-62 (2005).

    4. Clifford, J.J., and Waddington, J.L. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology 22(5), 538-544 (2000).