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Ro04-6790,5-HT6拮抗剂

Ro04-6790,5-HT6拮抗剂用途

Ro 04-6790 是一种有效的,竞争性和选择性的 5-HT6 受体拮抗剂,对大鼠和人的 5-HT6 受体的 pKi 值分别为 7.26、7.35。Ro 04-6790 对其他受体没有亲和力。

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Ro04-6790,5-HT6拮抗剂名称

[ CAS 号 ]:
202466-68-0

[ 中文名 ]:
4-氨基-N-[2,6-双(甲基氨基)-4-嘧啶基]-苯磺胺

[ 英文名 ]:
Ro 04-6790

[英文别名 ]:

Ro 04-6790

Ro04-6790,5-HT6拮抗剂生物活性

[ 描述 ]:

Ro 04-6790 是一种有效的,竞争性和选择性的 5-HT6 受体拮抗剂,对大鼠和人的 5-HT6 受体的 pKi 值分别为 7.26、7.35。Ro 04-6790 对其他受体没有亲和力。

[ 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 ]

Rat 5-HT6 Receptor:7.26 (pKi)

Human 5-HT6 Receptor:7.35 (pKi)

[体外研究]

与其他受体结合位点(IC50>10μM)相比,Ro 04-6790对5-HT6受体的选择性超过100倍[1]。

[体内研究]

Ro 04-6790(10 mg/kg,SC)使250-300 g成年雄性Wistar大鼠的ACh流出量适度增加(50%)(这一效应与载体的作用无统计学差异)[2]。

[参考文献]

[1]. A J Sleight, et al. Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors. Br J Pharmacol. 1998 Jun;124(3):556-62.

[2]. Sudabeh Shirazi-Southall, et al. Effects of typical and atypical antipsychotics and receptor selective compounds on acetylcholine efflux in the hippocampus of the rat. Neuropsychopharmacology. 2002 May;26(5):583-94.

Ro04-6790,5-HT6拮抗剂物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
595.8±60.0 °C at 760 mmHg

[ 分子式 ]:
C₁₂H₁₆N₆O₂S

[ 分子量 ]:
308.359

[ 闪点 ]:
314.1±32.9 °C

[ 精确质量 ]:
308.105530

[ PSA ]:
130.41000

[ LogP ]:
-0.52

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.700

[ 储存条件 ]:
-20°C，密封，干燥

Ro04-6790,5-HT6拮抗剂安全信息

[ 危害码 (欧洲) ]:
Xi

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

[ RTECS号 ]:
DA9462500

[ 海关编码 ]:
2935009090

Ro04-6790,5-HT6拮抗剂海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Ro04-6790,5-HT6拮抗剂文献

Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.

Br. J. Pharmacol. 124 , 556-562, (1998)

1. This study describes the in vitro characterization of two potent and selective 5-HT6 receptor antagonists at the rat and human recombinant 5-HT6 receptor. 2. In binding assays with [3H]-LSD, 4-amin...

Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats.

Br. J. Pharmacol. 126 , 1537-1542, (1999)

1. The present study examined the effects of the selective 5-HT6 receptor antagonist 4-amino-N-(2, 6 bis-methylamino-pyrimidin-4-yl)-benzene sulphonamide (Ro 04-6790) on locomotor activity and uncondi...

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