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PD 168077 maleate

Catalog No.GC17634

D4 dopamine receptor agonist

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PD 168077 maleate Chemical Structure

Cas No.: 630117-19-0

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10mg
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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Background

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It shows >100-fold selectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077 shows a 20-fold selectivity over α1, and α2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over 5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 receptor in terms of quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake in CHO cells expressing the human D4 receptor[1]. In the PD-168077-treated cell, p-CaMKII exhibits a significantly increased clustering at synaptic sites, as indicated by the enhanced colocalization with PSD-95[2].

PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced[1].

References:
[1]. Clifford JJ, et al. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology. 2000 May;22(5):538-44.
[2]. Gu Z, et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol Pharmacol. 2006 Mar;69(3):813-22.

Chemical Properties

Cas No. 630117-19-0 SDF
Chemical Name maleic acid compound with (Z)-N-((4-(2-cyanophenyl)piperazin-1-yl)methyl)-3-methylbenzimidic acid (1:1)
Canonical SMILES CC1=CC(/C(O)=N/CN2CCN(C3=CC=CC=C3C#N)CC2)=CC=C1.O=C(O)/C([H])=C([H])\C(O)=O
Formula C20H22N4O.C4H4O4 M.Wt 450.49
Solubility <11.26mg/ml in ethanol; <45.05mg/ml in DMSO Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2198 mL 11.099 mL 22.1981 mL
5 mM 0.444 mL 2.2198 mL 4.4396 mL
10 mM 0.222 mL 1.1099 mL 2.2198 mL
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