2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. RO5328673

RO5328673 是一种口服有效且能透过血脑屏障的神经激肽受体 (neurokinin receptor) 拮抗剂，可有效靶向人源 NK3 受体 ( Ki=0.4 nM，Ka=0.1 nM)、人源 NK2 受体 (Ki=1.1 nM，Ka=0.9 nM)、豚鼠 NK3 受体 (Ka=0.1 nM 和 0.13 nM)。RO5328673 具有独特的结合动力学特征，表现为 NK3 受体的不可克服型拮抗剂，具有缓慢的解离速率，而在人源 NK2 受体上则呈现快速的结合与解离速率。RO5328673 有效抑制 senktide (HY-P0187) 诱导的多巴胺能神经元自发活动增强，并逆转 senktide 诱导的沙鼠运动活性改变。RO5328673 可广泛应用于精神分裂症的相关研究。

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RO5328673

RO5328673 Chemical Structure

CAS No. : 1310817-94-7

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RO5328673 相关抗体

Top Publications Citing Use of Products

查看 Neurokinin Receptor 亚型特异性产品:

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NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia[1].

IC50 & Target

hNK2

1.1 nM (Ki)

hNK3

0.4 nM (Ki)

体外研究
(In Vitro)

RO5328673 (0.0003-10 μM) 可高亲和力结合 hNK2 和 hNK3 受体 (对应的 Ki 分别为 1.1 nM 和 0.4 nM)，与 hNK1 受体的亲和力较弱 (Ki 为 52.8 nM)[1]。
[3H]RO5328673 (0.01-20 nM; 23 °C (hNK2, hNK3, gpNK3) 或 37 °C (gpNK3)) 可高亲和力结合 hNK2、hNK3 和 gpNK3 受体上的单一饱和位点，且与 gpNK3 的结合具有温度非依赖性[1]。
RO5328673 (1-300 nM; 20 min) 是 hNK3 和 gpNK3 受体的不可克服性拮抗剂，可降低 [MePhe7]NKB 的最大反应强度和效能，且对 gpNK3 的作用更强[1]。

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

RO5328673 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Bioavailability CL Vss T1/2
Rat[1] 2 mg/kg i.v. / / 16 mL/min/kg 5 L/kg 3 h
Rat[1] 10 mg/kg p.o. 463 ng/mL 27 % / / /
体内研究
(In Vivo)

RO5328673 (10-30 mg/kg；口服) 可显著逆转 senktide (HY-P0187) 诱导的沙鼠运动活性异常[1]。

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

Animal Model: Mongolian gerbils (male and female, weight 40-70 g)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.
Result: Robustly reversed senktide-induced locomotor activity, with group mean total distance traveled reduced compared to vehicle-treated controls.
Produced plasma levels of 688 ng/mL (10 mg/kg dose) and 3508 ng/mL (30 mg/kg dose).
Produced brain levels of 360 ng/mL (10 mg/kg dose) and 1748 ng/mL (30 mg/kg dose).
Resulted in a brain/plasma ratio of 0.5 for both doses.
分子量

576.49

Formula

C29H32Cl2FN3O4
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

RO5328673 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

RO53286731310817-94-7RO 5328673RO-5328673Neurokinin ReceptorNK receptorTachykinin receptor[MePhe 7 ]NKBneurokinin receptor antagonistsenktidehuman NK2 receptorschizophreniahuman NK3 receptorguinea-pig NK3 receptordopaminergic neurongerbilhuman NK1 receptor
Inhibitorinhibitorinhibit

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HY-182423
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