PD-168077 maleate

SKU: orb1302141

Description

PD-168077 maleate is a potent and selective dopamine D4 receptor agonist with a Ki of 9 nM. This compound is a valuable research tool for investigating D4 receptor function in neuropsychiatric disorders, utilized in both in vitro binding assays and in vivo behavioral studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 630117-19-0
• MW: 450.49
• Purity: 99.13% (May vary between batches)
• Formula: C₂₄H₂₆N₄O₅
• SMILES: OC(=O)\C=C/C(O)=O.Cc1cccc(c1)C(=O)NCN1CCN(CC1)c1ccccc1C#N
• Target: Dopamine Receptor
• Solubility: DMSO:150 mg/mL (332.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.88 mM)

Bioactivity

• Target IC50:
  D4:9 nM(Ki)
• In Vivo:
  PD-168077, a selective D4 dopamine receptor agonist, injected into the paraventricular nucleus of the hypothalamus on penile erection was studied in male rats. PD-168077 (1-200 ng) induced penile erection in a dose-dependent manner. The minimal effective dose was 50 ng, while the maximal response was found with 200 ng of the compound, which increased penile erection episodes from 0.3+/-0.03 to 1.7+/-0.21. The proerectile effect of PD-168077 was reduced almost completely by L-745,870 (3-(4-[chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-B]pyridine trihydrochloride), a selective D4 dopamine receptor antagonist, (1 microg) given into the paraventricular nucleus before the D4 dopamine agonist, and by other nonselective dopamine receptor antagonists, such as haloperidol (1 microg) and clozapine (1 microg), which block all dopamine receptor subtypes. The pro-erectile effect of PD-168077 was also reduced by the NO synthase inhibitor NG-nitro-L-arginine methylester (25 microg), but not by the oxytocin receptor antagonist d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg), when given into the paraventricular nucleus. In spite of its inability to prevent the pro-erectile effect of PD-168077 when given in the paraventricular nucleus, d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg) reduced almost completely PD-168077-induced penile erection when given into the lateral ventricles.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

D4, Dopamine Receptor, DopamineReceptor, Dopamine, PD168077, PD-168077, PD168077 Maleate, PD168077 maleate, PD-168077 Maleate, PD 168077, PD 168077 Maleate, PD 168077 maleate, inhibit, Inhibitor

Compound Identifiers

PubChem CID

11957665