2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Dopamine Receptor CCR
  4. PNU-177864 hydrochloride

PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity.

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PNU-177864 hydrochloride Chemical Structure

PNU-177864 hydrochloride Chemical Structure

CAS No. : 1783978-03-9

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PNU-177864 hydrochloride Related Antibodies

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity[1][2][3].

IC50 & Target[1]

D3 Receptor

 

In Vitro

PNU-177864 (1-10 μM, 30 min) reduces CCR5 expression in THP1, reduces inflammation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PNU-177864 hydrochloride Related Antibodies
In Vivo

PNU-177864 (0-200 mg/kg,p.o., once daily for 2 weeks) can cause significant phospholipidosis and associated myopathy under certain conditions in rats, with plasma levels increasing throughout 24 hours at high doses. It remains high and almost unchanged over the dosing interval, but it has no obvious toxicity at lower doses[2].
PNU-177864 (0-200 mg/kg, p.o., once daily for 2 weeks) in rats and dogs is the accumulation of phospholipids in epididymal epithelial cells[3].
Pharmacokinetic analysis of oral PNU-177864 in rats[2]

Treatment (mg/kg/day) Day Cmax (μg/mL) Tmax (h) C24 (μg/mL) t1/2 (h) AUC0-24 (μg•h/mL) AUC0-∞ (ng•h/mL)
12.5 1 0.88 4-8 0.167 6.5 13.2 15.1
12.5 6 nc nc 0.23 nc nc nc
12.5 14 1.25 2-8 0.237 7.1 18.4 nc
50 1 3.64 8 1.84 16 63.9 117
50 6 nc nc 2.74 nc nc nc
50 14 5.7 4-8 2.50 13.7 104 nc
200 1 6.9 8-24 6.8 / 133 nc
200 6 nc nc 14.3 nc nc nc
200 11 15.9 0-8 11.06 / 306 nc

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female Sprague-Dawley rats (8-9-week-old)[1]
Dosage: 12.5 mg/kg, 50 mg/kg (for 2 weeks), or 200 mg/kg; 8 mg/kg, 25 mg/kg, or 80 mg/kg (for 4 weeks)
Administration: Oral gavage; daily; for 2-4 weeks
Result: Induced phospholipidosis in unusual target organs in dogs or rats including epididymis, pituitary, and hair follicles.
Animal Model: Male and female Sprague-Dawley rats (8-9-week-old)[1]
Dosage: 12.5 mg/kg, 50 mg/kg (for 2 weeks), or 200 mg/kg; 8 mg/kg, 25 mg/kg, or 80 mg/kg (for 4 weeks); daily; for 2-4 weeks
Administration: Oral
Result: Induced phospholipidosis in unusual target organs in dogs or rats including epididymis, pituitary, and hair follicles.
Animal Model: 9–10-month-old beagle dogs[3]
Dosage: 0, 2, 10, 50 mg/kg/day, 2 weeks; 0, 0.5, 4, 32 mg/kg/day, 4 weeks
Administration: Oral
Result: Showed lymphoid tissue (lymph nodes, foamy macrophages in the white medulla of the spleen or Peyer's patches), alveolar macrophages, epididymal epithelial cells, and peripheral blood lymphocytes showed changes consistent with phospholipidosis. After the recovery period, no histological and electron microscopic signs of phospholipidosis were found except in the epididymis.
Showed no histological changes were found in the epididymal epithelial cells; sperm density and morphology were normal histologically; the dogs had normal sperm concentration, morphology, and motility.
Molecular Weight

438.89

Formula

C18H22ClF3N2O3S
CAS No.
SMILES

O=S(C1=CC=C(OC(F)(F)F)C=C1)(NC2=CC=C(CCNCCC)C=C2)=O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PNU-177864 hydrochloride Related Classifications

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Keywords:

PNU-1778641783978-03-9PNU177864PNU 177864Dopamine ReceptorCCRCC chemokine receptorD3-receptorcationicamphiphilicphospholipidosisCADantischizophrenicmyopathyInhibitorinhibitorinhibit

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