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PD 168077 maleate

High affinity, selective D4 agonist CAS# 630117-19-0

PD 168077 maleate

Catalog No. BCC6919----Order now to get a substantial discount!

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Chemical structure

PD 168077 maleate

3D structure

Chemical Properties of PD 168077 maleate

Cas No. 630117-19-0 SDF Download SDF
PubChem ID 11957665 Appearance Powder
Formula C24H26N4O5 M.Wt 450.49
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 150 mg/mL (332.97 mM; Need ultrasonic)
Chemical Name (Z)-but-2-enedioic acid;N-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]-3-methylbenzamide
SMILES CC1=CC=CC(=C1)C(=O)NCN2CCN(CC2)C3=CC=CC=C3C#N.C(=CC(=O)O)C(=O)O
Standard InChIKey NAEUGRPISCANHO-BTJKTKAUSA-N
Standard InChI 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-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PD 168077 maleate

DescriptionA 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.

PD 168077 maleate Dilution Calculator

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PD 168077 maleate Molarity Calculator

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Preparing Stock Solutions of PD 168077 maleate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2198 mL 11.099 mL 22.1981 mL 44.3961 mL 55.4951 mL
5 mM 0.444 mL 2.2198 mL 4.4396 mL 8.8792 mL 11.099 mL
10 mM 0.222 mL 1.1099 mL 2.2198 mL 4.4396 mL 5.5495 mL
50 mM 0.0444 mL 0.222 mL 0.444 mL 0.8879 mL 1.1099 mL
100 mM 0.0222 mL 0.111 mL 0.222 mL 0.444 mL 0.555 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PD 168077 maleate

The novel dopamine D4 receptor agonist (PD 168,077 maleate): doses with different effects on locomotor activity are without effect in classical conditioning.[Pubmed:12691779]

Prog Neuropsychopharmacol Biol Psychiatry. 2003 May;27(3):441-9.

Conditioning is normally selective to the most likely predictors of motivationally significant events and some dopamine (DA) agonists produce dysfunction in this process. Moreover, the DA D(4) receptor is implicated in normal and abnormal functions that have some dopaminergic basis (e.g., in attention deficit hyperactivity disorder and schizophrenia). We therefore used locomotor activity to identify doses of a novel D(4) receptor agonist (PD 168,077) with contrasting behavioral effects (over the range 0.064-1 mg/kg). Doses that either did (0.064 mg/kg) or did not (0.5 mg/kg) significantly increase activity were then tested using aversive and appetitive procedures, in which conditioning was reflected in decreased and increased response rates, respectively. Associating a signal with food or foot shock is normally reduced in trace conditioning, when stimulus events are separated in time. Similarly, animals normally learn relatively little about background stimuli that do not well predict food delivery or the onset of shock. Both doses of PD 168,077 were without effect on conditioning, whether appetitive or aversive, and irrespective of how informative the predictive stimulus was. Thus, we find no evidence that the D(4) receptor has any likely effect on associative learning or its disorder. Furthermore, D(4)-mediated hyperactivity was dissociable from cognitive effects.

Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons.[Pubmed:16365279]

Mol Pharmacol. 2006 Mar;69(3):813-22.

One of the important targets of dopamine D4 receptors in prefrontal cortex (PFC) is the multifunctional Ca2+/calmodulin-dependent protein kinase II (CaMKII). In the present study, we investigated the effect of D4 receptor activation on subcellular localization of CaMKII. We found that activation of D4 receptors, but not D2 receptors, induced a rapid translocation of alpha-CaMKII from cytosol to postsynaptic sites in cultured PFC neurons. Activated CaMKII (Thr286 phospho-CaMKII) was also redistributed to postsynaptic sites after D4 receptor stimulation. The translocation was blocked by inhibiting the phospholipase C/inositol 1,4,5-trisphosphate receptor/Ca2+ signaling. Point mutation of the calmodulin binding site (Ala302), but not the autophosphorylation site (Thr286), of alpha-CaMKII prevented the D4-induced CaMKII translocation. Moreover, D4 receptors failed to induce CaMKII translocation in the presence of an actin stabilizer, and D4 activation reduced the binding of CaMKII to F-actin. Concomitant with the synaptic accumulation of alpha-CaMKII in response to D4 receptor activation, a D4-induced increase in the CaMKII phosphorylation of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor glutamate receptor 1 (GluR1) subunits and the amplitude of AMPA receptor-mediated excitatory postsynaptic currents was also observed. Thus, our results show that D4 receptor activation induces the synaptic translocation of CaMKII through a mechanism involving Ca2+/calmodulin and F-actin, which facilitates the regulation of synaptic targets of CaMKII, such as AMPA receptors.

Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists.[Pubmed:10731629]

Neuropsychopharmacology. 2000 May;22(5):538-44.

The effects of three selective D(4) antagonists [CP-293,019, L-745, 870, and Ro 61-6270] and two putative selective D(4) agonists [CP-226,269 and PD 168077] were compared with those of the generic D(2)-like [D(2L/S),D(3), D(4)] antagonist haloperidol to identify any characteristic "ethogram," in terms of individual topographies of behavior within the natural rodent repertoire, as evaluated using ethologically based approaches. Among the D(4) antagonists, neither L-745,870 (0.0016-1.0 mg/kg) nor Ro 61-6270 (0.2-25.0 mg/kg) influenced any behavior; whereas, CP-293,019 (0.2-25.0 mg/kg) induced episodes of nonstereotyped sniffing, sifting, and vacuous chewing; there were no consistent effects on responsivity to the D(2)-like agonist RU 24213. Among the putative D(4) agonists, CP-226, 269 (0.2-25.0 mg/kg) failed to influence any behavior; whereas, PD 168077 (0.2-25.0 mg/kg) induced nonstereotyped shuffling locomotion with uncoordinated movements, jerking, and yawning, which were insensitive to antagonism by CP-293,019, L-745,870, or haloperidol. These findings fail to indicate any "ethogram" for selective manipulation of D(4) receptor function at the level of the interaction between motoric and psychological processes in sculpting behavioral topography over habituation of exploration through to quiescence and focus attention on social, cognitive, or other levels of examination.

Description

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

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