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Cat. No.: HY-103406A

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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.

For research use only. We do not sell to patients.

CAS No.: 1783978-03-9
Formula: C₁₈H₂₂ClF₃N₂O₃S
Molecular Weight:438.89

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

PNU-177864 hydrochloride Chemical Structure

CAS No.: 1783978-03-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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

All Dopamine Receptor Isoforms :

All CCR Isoforms :

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.

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	C_max (μg/mL)	T_max (h)	C₂₄ (μg/mL)	t_1/2 (h)	AUC_0-24 (μg•h/mL)	AUC_0-∞ (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.

Chemical Information

CAS No. 1783978-03-9
Molecular Weight 438.89
Formula C₁₈H₂₂ClF₃N₂O₃S
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liana Basova , et al. Dopamine and its receptors play a role in the modulation of CCR5 expression in innate immune cells following exposure to Methamphetamine: Implications to HIV infection. PLoS One.2018 Jun 26;13(6):e0199861. [Content Brief]

[2]. Vonderfecht SL, et al. Myopathy related to administration of a cationic amphiphilic drug and the use of multidose drug distribution analysis to predict its occurrence. Toxicol Pathol. 2004 May-Jun;32(3):318-25. [Content Brief]

[3]. Rudmann DG, et al. Epididymal and systemic phospholipidosis in rats and dogs treated with the dopamine D3 selective antagonist PNU-177864. Toxicol Pathol. 2004 May-Jun;32(3):326-32. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PNU-177864 hydrochloride

All Dopamine Receptor Isoforms

All CCR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PNU-177864 hydrochloride Related Classifications

HY-103406A Related Classifications