PNU-177864 hydrochloride

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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 Estructura química

No. CAS : 1783978-03-9

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Other In-stock Forms of PNU-177864 hydrochloride:

PNU-177864

Other Forms of PNU-177864 hydrochloride:

PNU-177864 In-stock

Recomendaciones destacadas

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Dopamine Receptor:

Ver todas las isoformas

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

Ver todos los productos específicos de isoformas CCR:

Ver todas las isoformas

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

Actividad biológica
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Referencias
Revisión del cliente

Descripciòn

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.

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.

Peso molecular

438.89

Fòrmula

C₁₈H₂₂ClF₃N₂O₃S

No. CAS

1783978-03-9

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]