RO5328673
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.
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- CAS 番号: 1310817-94-7
- 分子式: C29H32Cl2FN3O4
- 分子量:576.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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hNK2 1.1 nM (Ki) |
hNK3 0.4 nM (Ki) |
RO5328673 (0.0003-10 μM) binds to hNK2 and hNK3 receptors with high affinity, with corresponding Ki values of 1.1 nM and 0.4 nM, respectively, while it shows weak affinity for the hNK1 receptor (Ki=52.8 nM)[1].
[3H]RO5328673 (0.01-20 nM; 23 °C for hNK2, hNK3, gpNK3 or 37 °C for gpNK3) binds with high affinity to a single saturable site on hNK2, hNK3 and gpNK3 receptors, and its binding to gpNK3 is temperature-independent[1].
RO5328673 (1-300 nM; 20 min) acts as an insurmountable antagonist of hNK3 and gpNK3 receptors, which reduces the maximal response intensity and potency of [MePhe7]NKB, with a stronger effect on gpNK3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongolian gerbils (male and female, weight 40-70 g)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.
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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.
化学情報
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CAS 番号 1310817-94-7
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分子量 576.49
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分子式 C29H32Cl2FN3O4
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SMILES
FC(C=C1)=CC=C1OC(N([C@H]2[C@H](C3=CC(Cl)=C(C=C3)Cl)CN(C2)C(C4CCN(CC4)C(C5(CC5)C)=O)=O)C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RO5328673 関連分類
HY-182423 関連分類
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