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Purity: ≥98%
PD-168077 maleate, the maleate salt of PD168077, is a novel, potent, centrally active and selective dopamine D4 receptor agonist with a Ki of 9 nM. Shows > 400-fold selectivity over D2 and > 300-fold selectivity versus D3 subtypes respectively.
| Targets |
Dopamine D4 receptor ( Ki = 9 nM )
Dopamine D₄ receptor (Ki = 9.0 nM), D₂ receptor (Ki = 3740 nM), D₃ receptor (Ki = 2810 nM) [1] |
|---|---|
| ln Vitro |
PD-168077 is among the initial agents discovered to be a potential selective D4 agonist. PD-168077 exhibits selectivity over other D2-like receptor family members and their D1-like counterparts by >100 fold; selectivity over α1, α2, 5-HT1A by 45 fold, and 5-HT2A receptors by 460 fold; quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake in CHO cells expressing the human D4 receptor[1] are examples of intrinsic activity at the D4 receptor. As seen by the improved colocalization with PSD-95, p-CaMKII shows a markedly increased clustering at synaptic sites in the PD-168077-treated cell[2].
In CHO cells expressing the human D₄ receptor, PD-168077 exhibits intrinsic activity as measured by quinpirole-like inhibition of forskolin-stimulated cAMP accumulation and stimulation of [³H]thymidine uptake. [1] |
| ln Vivo |
PD-168077 (0.2-25.0 mg/kg) causes a dose-dependent reduction in grooming and rearing while inducing a strange and distinctive "shuffling" form with yawning and erratic movements along with myoclonic jerking episodes[1].
In habituated rats, PD-168077 (0.2–25.0 mg/kg) induces non-stereotyped “shuffling” locomotion with uncoordinated movements, yawning, and episodes of myoclonic jerking; it also reduces grooming and rearing. These behaviors are not antagonized by D₄ antagonists (CP-293,019, L-745,870) or by the D₂-like antagonist haloperidol. [1] |
| Cell Assay |
The intrinsic activity of PD-168077 at the human D₄ receptor was assessed in CHO cells transfected with the receptor. Activity was measured via inhibition of forskolin-stimulated cAMP accumulation (similar to quinpirole) and stimulation of [³H]thymidine uptake. [1]
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| Animal Protocol |
Male Sprague-Dawley rats (180–350 g) were housed under controlled conditions. They were placed individually in observation cages and allowed to habituate for 3 hours before drug administration. PD-168077 was dissolved using ultrasonication in a minimum of glacial acetic acid, made up to volume with 40% cyclodextrin, and injected subcutaneously at a volume of 4 ml/kg. Behavioral assessments were performed using a 5-second time-sampling checklist over 15-minute intervals for up to 1 hour. [1]
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| References |
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| Additional Infomation |
PD-168077 is described as a putative selective D₄ receptor agonist with more than 100-fold selectivity for D₂-like and D₁-like receptors. It also exhibits additional selectivity for α₁, α₂, 5-HT₁A, and 5-HT₂A receptors. Its behavioral effects in rats suggest that its mechanism of action is not dopaminergic, and therefore caution should be exercised when using it as a D₄ receptor probe. [1]
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| Molecular Formula |
C24H26N4O5
|
|---|---|
| Molecular Weight |
450.4870
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| Exact Mass |
450.19
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| Elemental Analysis |
C, 63.99; H, 5.82; N, 12.44; O, 17.76
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| CAS # |
630117-19-0
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| Related CAS # |
190383-31-4; 630117-19-0
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| PubChem CID |
11957665
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
33
|
| Complexity |
610
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=C([H])C([H])=C([H])C(C([H])([H])[H])=C1[H])N([H])C([H])([H])N1C([H])([H])C([H])([H])N(C2=C([H])C([H])=C([H])C([H])=C2C#N)C([H])([H])C1([H])[H].O([H])C(/C(/[H])=C(/[H])\C(=O)O[H])=O
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| InChi Key |
NAEUGRPISCANHO-BTJKTKAUSA-N
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| 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-
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| Chemical Name |
(Z)-but-2-enedioic acid;N-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]-3-methylbenzamide
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| Synonyms |
PD-168077 maleate; PD168077 maleate; PD 168077 maleate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~150 mg/mL (~333 mM)
H2O: ≥ 0.1 mg/mL (~0.2 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2198 mL | 11.0990 mL | 22.1981 mL | |
| 5 mM | 0.4440 mL | 2.2198 mL | 4.4396 mL | |
| 10 mM | 0.2220 mL | 1.1099 mL | 2.2198 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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