2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor
  4. Paliperidone palmitate

Paliperidone palmitate  (Synonyms: 9-Hydroxyrisperidone palmitate)

目录号: HY-A0019A 纯度: 99.93%
COA 产品使用指南 技术支持

Paliperidone palmitate 是一种口服有效、可以通过血脑屏障的多巴胺 D2 受体和 5-羟色胺 2A (5-HT2A) 受体的竞争性拮抗剂。Paliperidone palmitate 通过与多巴胺 D2 受体和 5-HT2A 受体结合，竞争性地抑制多巴胺和 5-羟色胺的作用，调节神经递质系统的平衡，从而发挥抗精神病活性。Paliperidone palmitate 主要用于精神分裂症的研究。

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Paliperidone palmitate

Paliperidone palmitate Chemical Structure

CAS No. : 199739-10-1

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10 mg ￥175
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100 mg ￥693
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Customer Review

Other Forms of Paliperidone palmitate:

Paliperidone palmitate 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 5-HT Receptor 亚型特异性产品:

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia[1][2][3].

IC50 & Target[1]

D2 Receptor

 

5-HT2A Receptor

 

体内研究
(In Vivo)

Paliperidone palmitate (小鼠 62.4 mg/kg、大鼠 20 mg/kg；肌肉注射；单剂量) 在 BALB/c 小鼠和 Sprague Dawley 大鼠模型中，与透明质酸酶 (HY-172442) 联合给药会在注射后的前 4 天改变 Paliperidone palmitate 的 depot 释放，增加血浆暴露量，但不影响 Paliperidone palmitate 的长效释放特性。在小鼠中，透明质酸酶会改变注射部位的组织形态，使巨噬细胞在肌细胞间浸润，在大鼠中，注射部位会形成有中央腔和坏死的肉芽肿[2]。

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

Animal Model: BALB/c mice (female, about 20 g, 6-8 weeks old)+Sprague Dawley rats (male, about 250 g, 6-8 weeks old)[2]
Dosage: Mice: 62.4 mg/kg of Paliperidone palmitate, 5 U or 15 U of hyaluronidase (dissolved in normal saline)
Rats: 20 mg/kg of Paliperidone palmitate, 5 U or 15 U of Hyaluronidase (dissolved in phosphate buffered saline)
Administration: Intramuscular injection, single dose; for mice, 4-week study period; for rats, 21-28-day study period
Result: In mice, co-administration of hyaluronidase increased paliperidone plasma exposures in the first week after injection. The overall long-acting release nature of the formulation was maintained. Macrophages showed infiltration between individual myocytes when paliperidone palmitate was co-administered with hyaluronidase.
In rats, co-administration of hyaluronidase also increased exposure in the first 4 days, but the effect was less than that in mice. The long-acting exposure was still maintained for about 20 days. Co-administration of hyaluronidase did not discernably affect the granulomas or the surrounding myocytes in rats. The lymph node retention of paliperidone palmitate was diminished upon treatment with hyaluronidase in both mice and rats. The biphasic plasma concentration-time profiles of paliperidone in both species could be described by an open first-order disposition model with parallel fast and slow absorption processes.
The macrophage infiltration and angiogenesis at the injection site affected the drug release and absorption, and the effect of hyaluronidase on these processes was different between mice and rats.
分子量

664.89

Formula

C39H57FN4O4
CAS 号
性状

固体

颜色

White to off-white

运输条件

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

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

Ethanol 中的溶解度 : 2 mg/mL (3.01 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5040 mL 7.5200 mL 15.0401 mL
5 mM --- --- ---
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.93%

COA (283 KB) HNMR (358 KB) RP-HPLC (280 KB) MS (81 KB)

产品使用指南 (1538 KB)
参考文献

Paliperidone palmitate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 1.5040 mL 7.5200 mL 15.0401 mL 37.6002 mL
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:

Paliperidone199739-10-19-HydroxyrisperidoneDopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychoticesterprodrugschizophreniaatypicallong-actingInhibitorinhibitorinhibit

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