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- 详细信息
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
Tiapride Hydrochloride
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
51012-33-0
- 规格:
100mg/50mg/25mg
| 规格: | 100mg | 产品价格: | ¥734.0 |
|---|---|---|---|
| 规格: | 50mg | 产品价格: | ¥408.0 |
| 规格: | 25mg | 产品价格: | ¥262.0 |
| 基本信息 | |
| CAS | No.51012-33-0 |
| 中文名称 | 盐酸硫必利 |
| 英文名称 | Tiapride Hydrochloride |
| 分子式 | C15H25ClN2O4S |
| 分子量 | 364.89 |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| EC | EINECS 256-908-4 |
| MDL | MFCD00133861 |
| SMILES | CCN(CC)CCNC(=O)C1=C(C=CC(=C1)S(=O)(=O)C)OC.Cl |
| InChIKey | OTFDPNXIVHBTKW-UHFFFAOYSA-N |
| InChI | InChI=1S/C15H24N2O4S.ClH/c1-5-17(6-2)10-9-16-15(18)13-11-12(22(4,19)20)7-8-14(13)21-3;/h7-8,11H,5-6,9-10H2,1-4H3,(H,16,18);1H |
| PubChem CID | 5702214 |
| 靶点 | Dopamine Receptor |
| 通路 | Neuronal Signaling;GPCR & G Protein |
| 背景说明 | 是一种选择性的 D2 和 D3 多巴胺受体(D2 and D3 dopamine receptors)拮抗剂,具有抗运动障碍和抗焦虑活性,可用于神经安定剂的研究。 |
| 生物活性 | Tiapride Hydrochloride 是一种选择性口服的 D2 和 D3 多巴胺受体拮抗剂,IC50 值分别为 110-320 nM 和 180 nM,还具有镇静活性和抗焦虑活性。[1-2] |
| IC50 | D2 Receptor: 110-320nM(IC50);D3 Receptor: 180nM(IC50)[1] |
| In Vitro | Tiapride has affinity for dopamine D(2)(IC(50)= 110-320 nM)and D(3)(IC(50)= 180 nM)receptors in vitro but lacks affinity for dopamine D(1)and D(4)receptors and for non-dopaminergic receptors including H(1),alpha(1),alpha(2)-adrenergic and serotonergic receptors.[1] |
| 细胞实验 | Tiapride also shows dose-related inhibition of [3H]-raclopride binding in limbic areas and in the striatum of the rat in vivo(ED(50)approximately 20 mg/kg,ip). In microdialysis experiments,tiapride(over the range 10-30 mg/kg,ip)increased extracellular levels of dopamine in the nucleus accumbens and striatum. In behavioral experiments in rats,lower doses of tiapride(ED(50)= 10 mg/kg,ip)antagonised dopamine agonist-induced hyperactivity while higher doses(ED(50)= 60 mg/kg,ip)were required to block stereotyped movements. In addition,doses of tiapride up to 200 mg/kg,ip failed to induce catalepsy. In tests of conditioned behavior in rats,tiapride was found to give rise to an interoceptive stimulus associated with dopamine receptor blockade at doses(ED(50)= 2.2 mg/kg,ip)much lower than those producing motor disturbances or sedation(ED(50)= 40 mg/kg,ip).[1] |
| 数据来源文献 | [1]. Scatton B,et al. The preclinical pharmacologic profile of tiapride. Eur Psychiatry. 2001 Jan;16 Suppl 1:29s-34s. [2]. Peters DH,et al. Tiapride. A review of its pharmacology and therapeutic potential in the management of alcohol dependence syndrome. Drugs. 1994 Jun;47(6):1010-32. |
| 单位 | 瓶 |
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IT2530 盐酸硫必利 神经信号通路 索莱宝
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