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首页 / 抑制剂/激动剂 / 膜转运蛋白 / Glycine transporter / Bitopertin

比托派汀 /Bitopertin {[allProObj[0].p_purity_real_show]}

货号：A514249 同义名： 比拓喷丁 / RG1678;RO4917838

Bitopertin is a noncompetitive inhibitor of glycine reuptake with IC50 of 25 nM.

Bitopertin 化学结构 CAS号：845614-11-1
Bitopertin 化学结构
CAS号：845614-11-1
Bitopertin 3D分子结构
CAS号：845614-11-1
Bitopertin 化学结构 CAS号：845614-11-1
Bitopertin 3D分子结构 CAS号：845614-11-1
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Bitopertin 纯度/质量文件 产品仅供科研

货号：A514249 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Bitopertin 生物活性

靶点

  • GlyT1

    GlyT1, IC50:22 nM
描述 Bitopertin is a potent and noncompetitive glycine reuptake inhibitor targeting on GlyT1 (glycine transporter type 1), with IC50 value of 25nM. Bitopertin enhanced NMDA-dependent long-term potentiation at 100 nM but not at 300 nM in hippocampal CA1 pyramidal cells. It dose-dependently increased cerebrospinal fluid and striatal levels of glycine measured by microdialysis in rats. Also, it attenuated hyperlocomotion induced by the psychostimulant D-amphetamine or the NMDA receptor glycine site antagonist L-687,414 in mice. Additionally, it prevented the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker. Bitopertin is usually used in study of schizophrenia. It can modulate both glutamatergic and dopaminergic neurotransmission in animal experiments that model aspects of schizophrenia.
作用机制 Bitopertin could competitively block [3H]ORG24598 binding sites at human GlyT1b.[1]

Bitopertin 动物研究

Dose Mice: 0.1 mg/kg - 10 mg/kg[3] (i.p.); 0.3 mg/kg - 10 mg/kg[1] (p.o.) Rat: 0.3 mg/kg - 3 mg/kg[4] (p.o.), 1 mg/kg - 10 mg/kg[1] (p.o.)
Administration i.p., p.o.
Pharmacokinetics
Animal Rats[5] Monkeys[5]
Dose 2 mg/kg (i.v.)
3 mg/kg (p.o.) 		0.5 mg/kg (i.v.)
2.8 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o.
F 78% (p.o.) 56% (p.o.)
PPB % unbound 3
T1/2 5.8 h (p.o.) 6.4 h (p.o.)
Tmax 1 h (p.o.) 5.5 h (p.o.)
CL 4.32 ml/min/kg (i.v.) 3.62 ml/min/kg (i.v.)
Cmax 721 ng/ml (p.o.) 517 ng/ml (p.o.)
Vdss 3.58 L/kg (i.v.) 1.98 L/kg (i.v.)
AUC0→∞ 8670 ng·h/ml (p.o.) 7230 ng·h/ml (p.o.)
Protein binding (free drug %) 3

Bitopertin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01192906 Schizophrenia Phase 3 Completed - -
NCT01234779 Schizophrenia Phase 2 Completed - -
NCT01235559 Schizophrenia Phase 3 Completed - -

Bitopertin 参考文献

[1]Alberati D, Moreau JL, et al. Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia. Neuropharmacology. 2012 Feb;62(2):1152-61.

[2]Bugarski-Kirola D, Wang A, et al. A phase II/III trial of bitopertin monotherapy compared with placebo in patients with an acute exacerbation of schizophrenia - results from the CandleLyte study. Eur Neuropsychopharmacol. 2014 Jul;24(7):1024-36.

[3]Armbruster A, Neumann E, et al. The GlyT1 Inhibitor Bitopertin Ameliorates Allodynia and Hyperalgesia in Animal Models of Neuropathic and Inflammatory Pain. Front Mol Neurosci. 2018 Jan 10;10:438.

[4]Effects of Clozapine, Aripiprazole and Bitopertin in Rats Social Withdrawal Assessed in an Automatic Social Interaction Test

[5]Pinard E, Alanine A, et al. Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia. J Med Chem. 2010 Jun 24;53(12):4603-14.

Bitopertin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.20mL

1.84mL

0.92mL

18.40mL

3.68mL

1.84mL

Bitopertin 技术信息

CAS号845614-11-1
分子式C21H20F7N3O4S
分子量 543.455
别名 比拓喷丁 ;RG1678;RO4917838;R-1678
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(92 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Bitopertin | RG1678;RO4917838;R-1678 | 比拓喷丁 | Glycine transporter | AmBeed-信号通路专用抑制剂 | Bitopertin 纯度/质量文件 | Bitopertin 生物活性 | Bitopertin 动物研究 | Bitopertin 临床数据 | Bitopertin 参考文献 | Bitopertin 实验方案 | Bitopertin 技术信息

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