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

PNU-177864 是一种有效的，选择性的，口服活性的多巴胺 D3 受体拮抗剂。PNU-177864 可在体内诱导磷脂代谢，并具有抗精神分裂症活性。

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PNU-177864 hydrochloride Chemical Structure

PNU-177864 hydrochloride Chemical Structure

CAS No. : 1783978-03-9

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规格 是否有货
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100 mg   询价  
250 mg   询价  

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PNU-177864 hydrochloride 的其他形式现货产品:

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Other Forms of PNU-177864 hydrochloride:

PNU-177864 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

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

查看 CCR 亚型特异性产品:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

PNU-177864 (1-10 μM，30 min) 降低了 THP1 中 CCR5 的表达，减少炎症[1]。

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

PNU-177864 hydrochloride 相关抗体:
体内研究
(In Vivo)

PNU-177864 (0-200 mg/kg，口服，每天一次，两周) 在大鼠中在特定条件下能够引发显著的磷脂蓄积症及其相关肌病，高剂量下血浆水平在整个 24 小时给药间隔内保持较高且几乎不变，但其在较低剂量下无明显毒性[2]。
PNU-177864 (0-200 mg/kg，口服，每天一次，两周) 在大鼠和狗中最显著的表现是在附睾上皮细胞中出现磷脂蓄积[3]。
大鼠口服 PNU-177864 的药代动力学[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

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.
分子量

438.89

Formula

C18H22ClF3N2O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PNU-177864 hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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