富马酸依利色林

富马酸依利色林用途

依匹凡西林(SR-46349)半富马酸盐是一种有效、选择性和口服活性的5-HT2A受体拮抗剂,在大鼠皮质膜的IC50为5.8nm,Kd为1.14nm。与5-HT2B和5-HT2C[1][2]相比,半富马酸依匹凡西林对5-HT2A的选择性高出20倍以上。

富马酸依利色林名称

[ CAS 号 ]:
130580-02-8

[ 中文名 ]:
富马酸依利色林

[ 英文名 ]:
Eplivanserin hemifumarate

[英文别名 ]:

Eplivanserin hemifumarate
SR-46349 hemifumarate salt

富马酸依利色林生物活性

[ 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 ]

5-HT2A Receptor:5.8 nM (IC50)

5-HT2C Receptor:120 nM (IC50)

[体外研究]

半富马酸依哌凡西林(SR 46349B)对其他5-HT激酶表现出弱抑制作用,IC50为0.12μM(猪皮质5-HT1C)、14μM(大鼠海马5-HT1A)和16μM(大鼠stnatum 5-HT1B、牛尾状核5-HT1D)。依普伐舍林对大鼠皮质肾上腺素能α1和α2、大鼠全脑组胺H1、钠离子通道和大鼠纹状体多巴胺D1和D2也有抑制作用,IC50分别为3.4μM、1.0μM、5.0μM、39μM、9μM和28μM[1]。

[体内研究]

半富马酸依哌凡西林(SR 46349B)抑制[3H]酮西林的5-HT2受体结合,腹腔注射后ED50为0.087 mg/kg,腹腔注射后ED50为0.097 mg/kg[1]。SR 46349B(0.25-1 mg/kg；i、 p.)阻断大鼠重复可卡因治疗后可卡因诱发的多动症[2]。

[参考文献]

[1]. Rinaldi-Carmona M, et al. Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist. J Pharmacol Exp Ther. 1992 Aug;262(2):759-68.

[2]. Malgorzata Filip, et al. Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. J Pharmacol Exp Ther. 2004 Sep;310(3):1246-54.

富马酸依利色林物理化学性质

[ 沸点 ]:
456.3ºC at 760mmHg

[ 分子式 ]:
C₂₃H₂₅FN₂O₆

[ 分子量 ]:
444.45300

[ 闪点 ]:
229.8ºC

[ 精确质量 ]:
444.17000

[ PSA ]:
119.66000

[ LogP ]:
3.23880

[ 蒸汽压 ]:
1.63E-08mmHg at 25°C

富马酸依利色林MSDS

详细MSDS(安全技术说明书)

富马酸依利色林安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H410

[ 警示性声明 ]:
P273-P501

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

富马酸依利色林文献

Nest building is impaired in the Ts65Dn mouse model of Down syndrome and rescued by blocking 5HT2a receptors.

Neurobiol. Learn. Mem. 116 , 162-71, (2014)

Down syndrome (DS) has an incidence of about 1/700 births, and is therefore the most common cause of cognitive and behavioral impairments in children. Recent studies on mouse models of DS indicate tha...

Role of serotonin (5-HT)2 receptors in cocaine self-administration and seeking behavior in rats.

Pharmacol. Rep. 57(1) , 35-46, (2005)

Previous studies have indicated a role of serotonin (5-HT)2 receptors in modulation of the behavioral effects of cocaine. In the present study, the efficacy of SR 46349B (a 5-HT(2A) receptor antagonis...

Activation of slowly conducting medullary raphe-spinal neurons, including serotonergic neurons, increases cutaneous sympathetic vasomotor discharge in rabbit.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 288(4) , R909-18, (2005)

Neurons in the rostral medullary raphe/parapyramidal region regulate cutaneous sympathetic nerve discharge. Using focal electrical stimulation at different dorsoventral raphe/parapyramidal sites in an...

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