利坦丝林

利坦丝林用途

Ritanserin (R 55667) 是一种高效、相对选择性、可口服、长效的 5-HT2 受体拮抗剂,IC50 值为 0.9 nM,对组胺 Histamine H1,多巴胺 Dopamine D2,肾上腺素 Adrenergic α1,Adrenergic α2 受体的活性较弱。

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利坦丝林名称

[ CAS 号 ]:
87051-43-2

[ 中文名 ]:
利坦色林

[ 英文名 ]:
Ritanserin

[中文别名 ]:

利坦丝林

[英文别名 ]:

Ritanserinum
Ritanserina
Ritanserine
risperidone
Tiserton

利坦丝林生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

IC50: 0.9 nM (5-HT2 receptor), 35 nM (H1 receptor), 70 nM (D2 receptor), 97 nM (α1 receptor), 150 nM (α2 receptor)[1]

[体外研究]

Ritanserin(R 55667)是5-HT2受体的高效、相对选择性、长效拮抗剂,IC50为0.9nm,对组胺-h1(IC50,35nm)、多巴胺-d2(IC50,70nm)、肾上腺素能α1(IC50,97nm)、肾上腺素能α2受体(IC50,150nm)活性较低[1]。

[参考文献]

[1]. Leysen JE, et al. Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist. Mol Pharmacol. 1985 Jun;27(6):600-11.

利坦丝林物理化学性质

[ 密度 ]:
1.3g/cm3

[ 沸点 ]:
618.7ºC at 760 mmHg

[ 分子式 ]:
C₂₇H₂₅F₂N₃OS

[ 分子量 ]:
477.56900

[ 闪点 ]:
328ºC

[ 精确质量 ]:
477.16900

[ PSA ]:
65.85000

[ LogP ]:
5.42090

[ 折射率 ]:
1.646

[ 储存条件 ]:
室温，干燥

利坦丝林MSDS

详细MSDS(安全技术说明书)

利坦丝林安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 危险品运输编码 ]:
NONH for all modes of transport

利坦丝林文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).

J. Med. Chem. 51 , 3275-87, (2008)

The chemical space of registered oral drugs was explored for inhibitors of the human multidrug-resistance associated protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and dru...

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Nat. Chem. Biol. 5 , 765-71, (2009)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened...

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