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反式-6-氰基-3,4-二氢-2,2-二甲基-4-(2-氧吡咯啉-1-基)-2H-1-苯丙吡喃-3-醇

用途

GR 113808 是一种有效且高度选择性的 5-HT4 receptor 受体拮抗剂 (pKb= 8.8)。GR 113808 的选择性是 5-HT1A,5-HT1B,5-HT2A,5-HT2C 和 5-HT3 受体的 300 倍。

名称

[ CAS 号 ]:
144625-51-4

[ 中文名 ]:
1-[2-(METHYLSULFONYL)-AMINO]ETHYL-4-PIPERIDINYLMETHYL 1-METHYL-1H-INDOLE-3-CARBOXYLATE

[ 英文名 ]:
GR113808

[英文别名 ]:

Clocinnamox mesylate
MFCD00912901

生物活性

[ 描述 ]:

GR 113808 是一种有效且高度选择性的 5-HT4 receptor 受体拮抗剂 (pKb= 8.8)。GR 113808 的选择性是 5-HT1A,5-HT1B,5-HT2A,5-HT2C 和 5-HT3 受体的 300 倍。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

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

[体内研究]

GR113808(腹腔注射；1 mg/kg；诱导结肠炎后5-7天开始)显示疾病活动指数(DAI)显著增加,包括评估体重减轻、大便稠度和粪便血的存在[2]。动物模型：小鼠[1]剂量：1 mg/Kg给药：腹腔注射；1 mg/Kg；诱导结肠炎后5-7天开始给药。结果：替加色罗诱导结肠炎后保护作用受阻。

[参考文献]

[1]. Gale JD, et al. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.Br J Pharmacol. 1994 Jan;111(1):332-8.

[2]. Spohn SN, et al.Protective Actions of Epithelial 5-Hydroxytryptamine 4 Receptors in Normal and Inflamed Colon.Gastroenterology. 2016 Nov;151(5):933-944.e3.

物理化学性质

[ 密度 ]:
1.3g/cm3

[ 沸点 ]:
572.3ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₂₇N₃O₄S

[ 分子量 ]:
393.50000

[ 闪点 ]:
299.9ºC

[ 精确质量 ]:
393.17200

[ PSA ]:
89.02000

[ LogP ]:
3.00590

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
4.19E-13mmHg at 25°C

[ 折射率 ]:
1.613

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

文献

Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.

Bioorg. Med. Chem. 17 , 2607-2622, (2009)

Based on the definition of a 5-HT(4) receptor antagonist pharmacophore, a series of pyrrolo[1,2-a]thieno[3,2-e] and pyrrolo[1,2-a]thieno[2,3-e] pyrazine derivatives were designed, prepared, and evalua...

Dual role of serotonin in the pathogenesis of indomethacin-induced small intestinal ulceration: pro-ulcerogenic action via 5-HT3 receptors and anti-ulcerogenic action via 5-HT4 receptors.

Pharmacol. Res. 66(3) , 226-34, (2012)

Serotonin (5-HT) exerts multiple physiological functions not only in the central and peripheral nervous systems but also in the gastrointestinal tract, and these multiple functions are accounted for b...

Molecular characterization of a purified 5-HT4 receptor: a structural basis for drug efficacy.

J. Biol. Chem. 280(21) , 20253-60, (2005)

Serotonin 5-HT(4(a)) receptor, a G-protein-coupled receptor (GPCR), was produced as a functional isolated protein using Escherichia coli as an expression system. The isolated receptor was characterize...

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